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PMID:21226
|
Varicella-zoster virus-induced DNA polymerase.
|
Nuclear extracts of varicella-zoster virus (VZV)-infected human embryo lung (HEL) cells were found to contain DNA polymerase activity not present in uninfected HEL cells. This enzyme was designated the VZV-induced DNA polymerase. The VZV-induced polymerase was partially separated from the cellular alpha- and beta-polymerases by fractionation of the cells and by phosphocellulose chromatography. The separated enzymes were examined for the effect of added (NH4)2SO4, activity with synthetic templates, optimal pH, and the effect of phosphonoacetic acid. The VZV-induced DNA polymerase was distinct from cellular enzymes and had the properties of a typical herpesvirus-induced DNA polymerase.
|
Varicella-zoster virus-induced DNA polymerase. Nuclear extracts of varicella-zoster virus (VZV)-infected human embryo lung (HEL) cells were found to contain DNA polymerase activity not present in uninfected HEL cells. This enzyme was designated the VZV-induced DNA polymerase. The VZV-induced polymerase was partially separated from the cellular alpha- and beta-polymerases by fractionation of the cells and by phosphocellulose chromatography. The separated enzymes were examined for the effect of added (NH4)2SO4, activity with synthetic templates, optimal pH, and the effect of phosphonoacetic acid. The VZV-induced DNA polymerase was distinct from cellular enzymes and had the properties of a typical herpesvirus-induced DNA polymerase.
|
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] |
PMID:21227
|
[A new complex polymalformative syndrome (author's transl)].
|
The authors discuss the nosological position and the aetiology of a complex of malformations affecting a boy, born at the end of a 40-week pregnancy with a weight of 1420 g and height of 42.5 cm, who died at the age of 3 1/2 months. The case presented an association of an acrocephalosyndactyly, phalangeal hypoplasias with anonychia, aplasia of the abdominal muscles, a genital hypoplasia with cryptorchidism and hypospadias, patches of lipodystrophy localised on the outside of the arms, at the folds of the elbow and the popliteal fossae. The autopsy revealed a large interventricular communication, absence of common mesentery and especially important cerebral anomalies (smooth brain, absence of interhemispherical suture, disorganization of the basal ganglia). The genetic study suggested a spontaneous abortion 2 1/2 months before the birth of the patient and revealed, in the mother, the presence of bilateral clinodactylies of the fingers and a unilateral syndactyly of the big toes.
|
[A new complex polymalformative syndrome (author's transl)]. The authors discuss the nosological position and the aetiology of a complex of malformations affecting a boy, born at the end of a 40-week pregnancy with a weight of 1420 g and height of 42.5 cm, who died at the age of 3 1/2 months. The case presented an association of an acrocephalosyndactyly, phalangeal hypoplasias with anonychia, aplasia of the abdominal muscles, a genital hypoplasia with cryptorchidism and hypospadias, patches of lipodystrophy localised on the outside of the arms, at the folds of the elbow and the popliteal fossae. The autopsy revealed a large interventricular communication, absence of common mesentery and especially important cerebral anomalies (smooth brain, absence of interhemispherical suture, disorganization of the basal ganglia). The genetic study suggested a spontaneous abortion 2 1/2 months before the birth of the patient and revealed, in the mother, the presence of bilateral clinodactylies of the fingers and a unilateral syndactyly of the big toes.
|
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] |
PMID:21228
|
Brain tyrosine level controls striatal dopamine synthesis in haloperidol-treated rats.
|
Animals received either haloperidol (2 mg/kg) or probenecid (200 mg/kg) in conjunction with tyrosine (100 mg/kg) or its diluent. Striatal homovanillic acid levels increased in probenecid-treated animals to the same range whether they were given tyrosine or not. In haloperidol-treated animals the levels of homovanillic acid were significantly elevated in animals receiving tyrosine. Tyrosine and homovanillic acid levels were highly correlated as determined by linear regression analysis.
|
Brain tyrosine level controls striatal dopamine synthesis in haloperidol-treated rats. Animals received either haloperidol (2 mg/kg) or probenecid (200 mg/kg) in conjunction with tyrosine (100 mg/kg) or its diluent. Striatal homovanillic acid levels increased in probenecid-treated animals to the same range whether they were given tyrosine or not. In haloperidol-treated animals the levels of homovanillic acid were significantly elevated in animals receiving tyrosine. Tyrosine and homovanillic acid levels were highly correlated as determined by linear regression analysis.
|
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] |
PMID:21229
|
The interactions of bromocriptine and lergotrile with dopamine and alpha-adrenergic receptors.
|
Bromocriptine and lergotrile, which are clinically used as antiparkinsonian (AP) agents, compete for the binding of H3-dopamine, H3-apomorphine, and H3-haloperidol to striatal membrane sites. Lergotrile has a higher affinity for the H3-dopamine binding to bovine striatal membranes than bromocriptine. Lergotrile and bromocriptine are almost equipotent in competing for the binding of H3-apomorphine to rat striatal membranes, but bromocriptine is more potent in competing for the binding of H3-haloperidol than lergotrile. These results indicate that lergotrile and bromocriptine are mixed putative agonist-antagonist with respect to the postsynaptic dopamine receptors. Lergotrile and bromocriptine at higher concentrations inhibit synaptosomal tyrosine hydroxylase activity, and reverse the apomorphine elicited enzyme inhibition. Thus, these ergot alkaloids behave as mixed agonist-antagonist also with respect to the presynaptic dopamine receptors. Bromocriptine and lergotrile, as well as other tested DH-ergot alkaloids and neuroleptics, compete for the binding of the alpha-antagonist H3-WB-4101 to rat cerebral cortical membranes. The displacing potencies of the tested DH-ergot alkaloids and of the neuroleptics indicate that they have a high affinity for the alpha-adrenoreceptors in the CNS.
|
The interactions of bromocriptine and lergotrile with dopamine and alpha-adrenergic receptors. Bromocriptine and lergotrile, which are clinically used as antiparkinsonian (AP) agents, compete for the binding of H3-dopamine, H3-apomorphine, and H3-haloperidol to striatal membrane sites. Lergotrile has a higher affinity for the H3-dopamine binding to bovine striatal membranes than bromocriptine. Lergotrile and bromocriptine are almost equipotent in competing for the binding of H3-apomorphine to rat striatal membranes, but bromocriptine is more potent in competing for the binding of H3-haloperidol than lergotrile. These results indicate that lergotrile and bromocriptine are mixed putative agonist-antagonist with respect to the postsynaptic dopamine receptors. Lergotrile and bromocriptine at higher concentrations inhibit synaptosomal tyrosine hydroxylase activity, and reverse the apomorphine elicited enzyme inhibition. Thus, these ergot alkaloids behave as mixed agonist-antagonist also with respect to the presynaptic dopamine receptors. Bromocriptine and lergotrile, as well as other tested DH-ergot alkaloids and neuroleptics, compete for the binding of the alpha-antagonist H3-WB-4101 to rat cerebral cortical membranes. The displacing potencies of the tested DH-ergot alkaloids and of the neuroleptics indicate that they have a high affinity for the alpha-adrenoreceptors in the CNS.
|
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] |
PMID:21230
|
Comparison of gamma-glutamyl transpeptidase activity in tissues of normal and dystrophic hamsters and mice.
|
The activity of gamma-glutamyl transpeptidase (gamma-GT), a membrane-bound enzyme, was assayed by a sensitive fluorometric method in the brain, heart, kidney, liver, skeletal muscle and serum of normal and dystrophic hamsters and mice. Normal and dystrophic hamsters were of the golden brown and BIO 14.6 line respectively. Both normal and dystrophic mice were of the C57 BL/6J -dy2j strain. Kidneys of both hamsters and mice contained the highest enzyme activity followed by the brain, skeletal muscle, liver and heart. Gamma-GT activity was elevated in dystrophic skeletal muscles but decreased in the dystrophic kidneys and sera. In the brain, heart and liver of dystrophic animals from both species enzyme activity was similar to that in normals.
|
Comparison of gamma-glutamyl transpeptidase activity in tissues of normal and dystrophic hamsters and mice. The activity of gamma-glutamyl transpeptidase (gamma-GT), a membrane-bound enzyme, was assayed by a sensitive fluorometric method in the brain, heart, kidney, liver, skeletal muscle and serum of normal and dystrophic hamsters and mice. Normal and dystrophic hamsters were of the golden brown and BIO 14.6 line respectively. Both normal and dystrophic mice were of the C57 BL/6J -dy2j strain. Kidneys of both hamsters and mice contained the highest enzyme activity followed by the brain, skeletal muscle, liver and heart. Gamma-GT activity was elevated in dystrophic skeletal muscles but decreased in the dystrophic kidneys and sera. In the brain, heart and liver of dystrophic animals from both species enzyme activity was similar to that in normals.
|
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] |
PMID:21231
|
8alpha-hydroxyflavinmononucleotide and related compounds.
|
2', 3', 4'-Triacetyl-FMN has been transformed by selective radical bromination into 2', 3', 4'-triacetyl-8alpha-bromo-FMN, and the following hydrolysis of the latter has afforded 8alpha-hydroxy-FMN. The presence of the hydroxy group in the 8alpha position of 8alpha-hydroxy-FMN is confirmed by its acetylation into 2', 3'-diacetyl-8alpha-acetoxyriboflavin-4', 5'-cyclophosphate. The absorption spectra of the synthesized compounds have shown the reduction of the extinction ratios of the first and second absorption maxima in comparison with the extinction of the same maxima for 8alpha-hydroxyriboflavin. Unlike FMN, fluorescence quenching for 8alpha-hydroxy-FMN has been found.
|
8alpha-hydroxyflavinmononucleotide and related compounds. 2', 3', 4'-Triacetyl-FMN has been transformed by selective radical bromination into 2', 3', 4'-triacetyl-8alpha-bromo-FMN, and the following hydrolysis of the latter has afforded 8alpha-hydroxy-FMN. The presence of the hydroxy group in the 8alpha position of 8alpha-hydroxy-FMN is confirmed by its acetylation into 2', 3'-diacetyl-8alpha-acetoxyriboflavin-4', 5'-cyclophosphate. The absorption spectra of the synthesized compounds have shown the reduction of the extinction ratios of the first and second absorption maxima in comparison with the extinction of the same maxima for 8alpha-hydroxyriboflavin. Unlike FMN, fluorescence quenching for 8alpha-hydroxy-FMN has been found.
|
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] |
PMID:21232
|
The presence and possible function of methylmalonyl CoA mutase and propionyl CoA carboxylase in Spirometra mansonoides.
|
Both spargana and adult forms of Spirometra mansonoides were shown to accumulate lactate, succinate, acetate, and propionate upon in vitro incubation. Adults differed markedly from the spargana in that quantitatively the most significant products of the former were acetate and propionate while the latter formed primarily acetate and lactate. The adults accumulated approximately 32 times more propionate than the spargana per gram of tissue. In accord with this propionate formation, propionyl CoA carboxylase and methylmalonyl CoA mutase have been found to be present in both stages of the parasite. As might be predicted, however, the activities of the carboxylase and mutase were 100-fold and 10-fold higher, respectively, in the adults as compared to the larvae. A possible physiological relationship between propionate formation and energy generation is suggested. Accordingly, inorganic 32P was incorporated into ATP upon incubation of methylmalonyl CoA with a homogenate obtained from adult S. mansonoides. Since methylmalonyl CoA mutase requires vitamin B12 coenzyme, a relationship between vitamin B12 content and propionate formation in helminths is suggested.
|
The presence and possible function of methylmalonyl CoA mutase and propionyl CoA carboxylase in Spirometra mansonoides. Both spargana and adult forms of Spirometra mansonoides were shown to accumulate lactate, succinate, acetate, and propionate upon in vitro incubation. Adults differed markedly from the spargana in that quantitatively the most significant products of the former were acetate and propionate while the latter formed primarily acetate and lactate. The adults accumulated approximately 32 times more propionate than the spargana per gram of tissue. In accord with this propionate formation, propionyl CoA carboxylase and methylmalonyl CoA mutase have been found to be present in both stages of the parasite. As might be predicted, however, the activities of the carboxylase and mutase were 100-fold and 10-fold higher, respectively, in the adults as compared to the larvae. A possible physiological relationship between propionate formation and energy generation is suggested. Accordingly, inorganic 32P was incorporated into ATP upon incubation of methylmalonyl CoA with a homogenate obtained from adult S. mansonoides. Since methylmalonyl CoA mutase requires vitamin B12 coenzyme, a relationship between vitamin B12 content and propionate formation in helminths is suggested.
|
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] |
PMID:21235
|
A comparison of the dissolution rates of caffeine tablets in a rotating-basket with those in a Sartorius dissolution tester.
|
Uncoated caffeine tablets of four different hardnesses were tested for dissolution rate by the Sartorius (S.S. method) and by the rotating basket method of the U.S.P. XVIII. In both methods the dissolution rate decreased with increasing hardness, and the rate obtained with the S.S. method was always less than that by the U.S.P. method. This result cannot be explained as being due only to the difference in the volume of dissolution medium. Also it was difficult to ensure that the characteristic changes in the process of dissolution paralleled the curves obtained from a plot of % caffeine dissolved vs time. Accordingly, the dissolution rate constants were calculated from the slope of each straight line in a plot of ln W infinity/(W infinity --W) vs time.
|
A comparison of the dissolution rates of caffeine tablets in a rotating-basket with those in a Sartorius dissolution tester. Uncoated caffeine tablets of four different hardnesses were tested for dissolution rate by the Sartorius (S.S. method) and by the rotating basket method of the U.S.P. XVIII. In both methods the dissolution rate decreased with increasing hardness, and the rate obtained with the S.S. method was always less than that by the U.S.P. method. This result cannot be explained as being due only to the difference in the volume of dissolution medium. Also it was difficult to ensure that the characteristic changes in the process of dissolution paralleled the curves obtained from a plot of % caffeine dissolved vs time. Accordingly, the dissolution rate constants were calculated from the slope of each straight line in a plot of ln W infinity/(W infinity --W) vs time.
|
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] |
PMID:21236
|
Plasma concentrations and excretion of zipeprol in man under acidic urine conditions.
|
Plasma concentrations of zipeprol, and the urinary excretion of it and two of its basic metabolites, compound II and compound III were examined after oral administration of zipeprol hydrochloride to man. The drug was rapidly and extensively metabolized, and the amount of unchanged drug excreted in the acidic urine varied from 1-5% of the dose; the two basic metabolites accounted for 19-38% of the dose.
|
Plasma concentrations and excretion of zipeprol in man under acidic urine conditions. Plasma concentrations of zipeprol, and the urinary excretion of it and two of its basic metabolites, compound II and compound III were examined after oral administration of zipeprol hydrochloride to man. The drug was rapidly and extensively metabolized, and the amount of unchanged drug excreted in the acidic urine varied from 1-5% of the dose; the two basic metabolites accounted for 19-38% of the dose.
|
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] |
PMID:21237
|
The effect of age and thyroid hormones upon the ability of the chick heart to deaminate monoamines.
|
The effect of age and thyroid hormones upon the ability of chick heart homogenates to metabolize monoamines has been investigated. 5-Hydroxytryptamine is entirely metabolized by a monoamine oxidase (MAO) with the characteristics of MAO-A, whereas some of the tyramine and all of the benzylamine are oxidatively deaminated by a clorgyline-resistant, but semicarbazide-sensitive enzyme, with a similar subcellular distribution to that of MAO. The remainder of the tyramine deamination is brought about by MAO-A and MAO-B. The specific activities of both clorgyline-sensitive and resistant enzymes are increased by the same proportion by increase in age or by treatment with (--)-thyroxine, and decreased by 2-thiouracil. The significance of these results is discussed.
|
The effect of age and thyroid hormones upon the ability of the chick heart to deaminate monoamines. The effect of age and thyroid hormones upon the ability of chick heart homogenates to metabolize monoamines has been investigated. 5-Hydroxytryptamine is entirely metabolized by a monoamine oxidase (MAO) with the characteristics of MAO-A, whereas some of the tyramine and all of the benzylamine are oxidatively deaminated by a clorgyline-resistant, but semicarbazide-sensitive enzyme, with a similar subcellular distribution to that of MAO. The remainder of the tyramine deamination is brought about by MAO-A and MAO-B. The specific activities of both clorgyline-sensitive and resistant enzymes are increased by the same proportion by increase in age or by treatment with (--)-thyroxine, and decreased by 2-thiouracil. The significance of these results is discussed.
|
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] |
PMID:21238
|
Evidence from agonist and antagonist studies to suggest that the beta1-adrenoceptors subserving the positive inotropic and chronotropic responses of the heart do not belong to two separate subgroups.
|
The positive inotropic and chronotropic responses of guinea-pig isolated left and right atria to 17 sympathomimetic amines were examined under conditions selected to control the pharmacological environment. Each agonist was compared with (--)-isoprenaline as the reference by constructing dose-response curves. Equiactive molar concentration ratios relative to (--)-isoprenaline were calculated at the EC50 for rate and tension responses. Statistical analysis revealed that (--)-noradrenaline and (+/-)-alpha-methylnoradrenaline were tension selective whereas (+/-)-alpha-ethylisoprenaline and N-methyldopamine were rate selective relative to (--)-isoprenaline. However, no structural trends emerged. The rank order of potency varied slightly between rate and tension, but an analysis of the regression and correlation coefficients indicated respectively that the equiactive molar concentration ratios and the rank orders could be considered identical on rate and tension. Antagonism of the (--)-isoprenaline-induced rate and tension responses by acebutolol, atenolol, practolol and propranolol was assessed from the pA2 values which were almost identical for both parameters with each antagnosti. It is concluded that the beta1-adrenoceptors mediating the positive inotropic and chronotropic responses do not warrant subdivision into two separate groups.
|
Evidence from agonist and antagonist studies to suggest that the beta1-adrenoceptors subserving the positive inotropic and chronotropic responses of the heart do not belong to two separate subgroups. The positive inotropic and chronotropic responses of guinea-pig isolated left and right atria to 17 sympathomimetic amines were examined under conditions selected to control the pharmacological environment. Each agonist was compared with (--)-isoprenaline as the reference by constructing dose-response curves. Equiactive molar concentration ratios relative to (--)-isoprenaline were calculated at the EC50 for rate and tension responses. Statistical analysis revealed that (--)-noradrenaline and (+/-)-alpha-methylnoradrenaline were tension selective whereas (+/-)-alpha-ethylisoprenaline and N-methyldopamine were rate selective relative to (--)-isoprenaline. However, no structural trends emerged. The rank order of potency varied slightly between rate and tension, but an analysis of the regression and correlation coefficients indicated respectively that the equiactive molar concentration ratios and the rank orders could be considered identical on rate and tension. Antagonism of the (--)-isoprenaline-induced rate and tension responses by acebutolol, atenolol, practolol and propranolol was assessed from the pA2 values which were almost identical for both parameters with each antagnosti. It is concluded that the beta1-adrenoceptors mediating the positive inotropic and chronotropic responses do not warrant subdivision into two separate groups.
|
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] |
PMID:21239
|
The role of dopaminergic systems in gamma-hydroxybutyrate-induced electrocorticogram hypersynchronization in the rat.
|
The effects of dopaminergic agonists and antagonists on the duration of hypersynchronization induced in the electrocorticogram (ecog) by gamma-hydroxybutyrate (gamma-HB) were tested in rats. Apomorphine (0-2-8 mg kg-1), piribedil (2-5-10 mg kt-1) and haloperidol (0-5-1 mg kg-1) had no influence on the duration of the hypersynchrony. Amphetamine (1-5-6 mg kg-1) inhibited the hypersynchrony, while (3,4-dihydroxyphenylamino)-2-imidazoline (DPI; 5, but not 1, mg kg-1) prolonged its duration. The lack of effect of the dopamine receptor agonists apomorphine and piribedil, and the dopamine receptor blocker haloperidol, on the gamma-HB-induced hypersynchrony might indicate that the inhibition of the impulse flow in the nigrostriatal dopamine system by gamma-HB is not involved in the generation of the hypersynchrony. DPI is thought to be an agonist at a dopamine receptor not sensitive to apomorphine, and its facilitatory effect on gamam-HB-hypersynchrony can be interpreted in terms of a possible involvement of another dopamine system in the ecog hypersynchrony induced by gamma-HB. The antagonism of gamma-HB by amphetamine is possibly due to an indirect stimulatory effect on noradrenergic receptors.
|
The role of dopaminergic systems in gamma-hydroxybutyrate-induced electrocorticogram hypersynchronization in the rat. The effects of dopaminergic agonists and antagonists on the duration of hypersynchronization induced in the electrocorticogram (ecog) by gamma-hydroxybutyrate (gamma-HB) were tested in rats. Apomorphine (0-2-8 mg kg-1), piribedil (2-5-10 mg kt-1) and haloperidol (0-5-1 mg kg-1) had no influence on the duration of the hypersynchrony. Amphetamine (1-5-6 mg kg-1) inhibited the hypersynchrony, while (3,4-dihydroxyphenylamino)-2-imidazoline (DPI; 5, but not 1, mg kg-1) prolonged its duration. The lack of effect of the dopamine receptor agonists apomorphine and piribedil, and the dopamine receptor blocker haloperidol, on the gamma-HB-induced hypersynchrony might indicate that the inhibition of the impulse flow in the nigrostriatal dopamine system by gamma-HB is not involved in the generation of the hypersynchrony. DPI is thought to be an agonist at a dopamine receptor not sensitive to apomorphine, and its facilitatory effect on gamam-HB-hypersynchrony can be interpreted in terms of a possible involvement of another dopamine system in the ecog hypersynchrony induced by gamma-HB. The antagonism of gamma-HB by amphetamine is possibly due to an indirect stimulatory effect on noradrenergic receptors.
|
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] |
PMID:21240
|
The central and peripheral effectiveness of two oxotremorine-antagonists determined using oxotremorine-induced tremor and salivation.
|
Two oxotremorine antagonists have been examined using oxotremorine as the tremor salivation inducer and the ratios between the central and peripheral nervous systems determined. Under these conditions these compounds are still more effective antagonists centrally than peripherally. Differences in distribution to the various muscarinic receptors involved is believed to be the major factor in determining this separation of central and peripheral activities.
|
The central and peripheral effectiveness of two oxotremorine-antagonists determined using oxotremorine-induced tremor and salivation. Two oxotremorine antagonists have been examined using oxotremorine as the tremor salivation inducer and the ratios between the central and peripheral nervous systems determined. Under these conditions these compounds are still more effective antagonists centrally than peripherally. Differences in distribution to the various muscarinic receptors involved is believed to be the major factor in determining this separation of central and peripheral activities.
|
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] |
PMID:21241
|
A sex difference in the interaction between promethazine and morphine in the mouse.
|
The effects of promethazine on the antinociceptive and respiratory actions of morphine have been examined in the mouse. Moderate doses of promethazine (5 and 10 mg kg-1) potentiated morphine's action in male mice but inhibited it in female mice. Gonadectomy abolished the interaction between promethazine and morphine in both sexes, although the intensity and duration of morphine's activity was greatly enhanced in these mice. Replacement of oestradiol in ovariectomized mice restored morphine's activity to intact female control values. However, interactions between promethazine and morphine required progesterone, as well as oestradiol, replacement to obtain results approaching those obtained in intact female mice.
|
A sex difference in the interaction between promethazine and morphine in the mouse. The effects of promethazine on the antinociceptive and respiratory actions of morphine have been examined in the mouse. Moderate doses of promethazine (5 and 10 mg kg-1) potentiated morphine's action in male mice but inhibited it in female mice. Gonadectomy abolished the interaction between promethazine and morphine in both sexes, although the intensity and duration of morphine's activity was greatly enhanced in these mice. Replacement of oestradiol in ovariectomized mice restored morphine's activity to intact female control values. However, interactions between promethazine and morphine required progesterone, as well as oestradiol, replacement to obtain results approaching those obtained in intact female mice.
|
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] |
PMID:21242
|
Some antagonists of dantrolene sodium on the isolated diaphragm muscle of the rat.
|
The effects of a number of potential antagonists of dantrolene sodium have been studied on twitches of the isolated hemidiaphragm preparation of the rat stimulated directly at a frequency of 0-1 Hz, after complete neuromuscular block produced by tubocurarine or erabutoxin a. The substances selected as possible dantrolene antagonists were uranyl ions, thiocyanate ions, adrenaline, caffeine, quazodine, quinine, 4-aminopyridine and the calcium ionophore a23187, all of which facilitate excitation-contraction coupling in one way or another. Contracture was the main feature of the response to A23187, the increase in the tension of the dantrolene-depressed twitches being very slight. All the remaining compounds increased the amplitude of the twitches, but only 4-aminopyridine, quinine, quazodine and caffeine were capable of restoring to the control amplitude twitches that had been maximally depressed by dantrolene. OF these, 4-aminopyridine and quinine were the most potent on a molar basis.
|
Some antagonists of dantrolene sodium on the isolated diaphragm muscle of the rat. The effects of a number of potential antagonists of dantrolene sodium have been studied on twitches of the isolated hemidiaphragm preparation of the rat stimulated directly at a frequency of 0-1 Hz, after complete neuromuscular block produced by tubocurarine or erabutoxin a. The substances selected as possible dantrolene antagonists were uranyl ions, thiocyanate ions, adrenaline, caffeine, quazodine, quinine, 4-aminopyridine and the calcium ionophore a23187, all of which facilitate excitation-contraction coupling in one way or another. Contracture was the main feature of the response to A23187, the increase in the tension of the dantrolene-depressed twitches being very slight. All the remaining compounds increased the amplitude of the twitches, but only 4-aminopyridine, quinine, quazodine and caffeine were capable of restoring to the control amplitude twitches that had been maximally depressed by dantrolene. OF these, 4-aminopyridine and quinine were the most potent on a molar basis.
|
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] |
PMID:21254
|
The dissolution mechanism in a system undergoing complexation: salicylamide in caffeine solution.
|
The dissolution rate of compressed salicylamide discs has been measured in water and in caffeine solutions of increasing concentration at 15, 25, 37 and 45 degrees in an apparatus rotating at 48 rev min-1 or more. Dissolution rate profiles showed breaks indicative of a shift in the mechanism of dissolution from interfacial towards transport control. The shifts occurred at higher caffeine concentrations on increasing the agitation rate or temperature. The dependencies of dissolution rates on agitation rates typified the intermediate type of dissolution and Arrhenius plots indicated that interfacial and transport processes participated in salicylamide dissolution.
|
The dissolution mechanism in a system undergoing complexation: salicylamide in caffeine solution. The dissolution rate of compressed salicylamide discs has been measured in water and in caffeine solutions of increasing concentration at 15, 25, 37 and 45 degrees in an apparatus rotating at 48 rev min-1 or more. Dissolution rate profiles showed breaks indicative of a shift in the mechanism of dissolution from interfacial towards transport control. The shifts occurred at higher caffeine concentrations on increasing the agitation rate or temperature. The dependencies of dissolution rates on agitation rates typified the intermediate type of dissolution and Arrhenius plots indicated that interfacial and transport processes participated in salicylamide dissolution.
|
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] |
PMID:21255
|
Dilute solution properties of clindamycin 2-palmitate hydrochloride.
|
Clindamycin 2-palmitate hydrochloride forms micelles in aqueous solution at concentrations above 2-2 X 10(-3) M. Dilution of micellar solutions of the drug to concentrations less than 2-0 X 10(-3) M produces turbid systems. Turbidity is caused by unionized drug, produced by hydrolysis of the salt, phasing out of solution at concentrations too low for micelles to be formed. Changes in specific conductivity and turbidity associated with the phasing-out process have been measured and explained in terms of the rates of the various processes involved, including demicellization and emulsion stability. The phenomenon of phasing-out, below a critical concentration in aqueous solution, is predicted to be a general one for weakly ionized surfactants where the unionized species possesses low water solubility.
|
Dilute solution properties of clindamycin 2-palmitate hydrochloride. Clindamycin 2-palmitate hydrochloride forms micelles in aqueous solution at concentrations above 2-2 X 10(-3) M. Dilution of micellar solutions of the drug to concentrations less than 2-0 X 10(-3) M produces turbid systems. Turbidity is caused by unionized drug, produced by hydrolysis of the salt, phasing out of solution at concentrations too low for micelles to be formed. Changes in specific conductivity and turbidity associated with the phasing-out process have been measured and explained in terms of the rates of the various processes involved, including demicellization and emulsion stability. The phenomenon of phasing-out, below a critical concentration in aqueous solution, is predicted to be a general one for weakly ionized surfactants where the unionized species possesses low water solubility.
|
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] |
PMID:21256
|
Relaxations mediated by adrenergic and non-adrenergic nerves in human isolated taenia coli.
|
In human taenia coli electrical field stimulation after cholinergic blockade excited mainly non-adrenergic inhibitory nerves. Adrenergic relaxations during stimulation were demonstrated only with short electrical pulses at high frequencies or with ganglion stimulants. Reduction by tetrodotoxin of relaxations to indirectly acting sympathomimetics supports the histochemical finding that colonic adrenergic nerves are mainly preganglionic, and possibly synapse with non-adrenergic inhibitory nerves. When the latter undergo direct maximal stimulation, responses to adrenergic nerve excitation are masked.
|
Relaxations mediated by adrenergic and non-adrenergic nerves in human isolated taenia coli. In human taenia coli electrical field stimulation after cholinergic blockade excited mainly non-adrenergic inhibitory nerves. Adrenergic relaxations during stimulation were demonstrated only with short electrical pulses at high frequencies or with ganglion stimulants. Reduction by tetrodotoxin of relaxations to indirectly acting sympathomimetics supports the histochemical finding that colonic adrenergic nerves are mainly preganglionic, and possibly synapse with non-adrenergic inhibitory nerves. When the latter undergo direct maximal stimulation, responses to adrenergic nerve excitation are masked.
|
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] |
PMID:21257
|
Evidence for more than one type of 5-hydroxytryptamine receptor in the human colon.
|
The actions of methysergide, a 5-hydroxytryptamine (5-HT) antagonist, have been examined on muscle strips taken from the circular and longitudinal layers of the human colon. Relaxations of the longitudinal muscle to 5-HT were antagonized by concentrations of methysergide known to be selective. Relaxations of the circular muscle to 5-HT were unaffected by similar concentrations of methysergide. Responses of both types of muscle to 5-HT were partially reduced by tetrodotoxin. Furthermore there was evidence for 5-HT receptors in circular colonic muscle which were unaffected either by selective concentrations of methysergide or tetrodotoxin.
|
Evidence for more than one type of 5-hydroxytryptamine receptor in the human colon. The actions of methysergide, a 5-hydroxytryptamine (5-HT) antagonist, have been examined on muscle strips taken from the circular and longitudinal layers of the human colon. Relaxations of the longitudinal muscle to 5-HT were antagonized by concentrations of methysergide known to be selective. Relaxations of the circular muscle to 5-HT were unaffected by similar concentrations of methysergide. Responses of both types of muscle to 5-HT were partially reduced by tetrodotoxin. Furthermore there was evidence for 5-HT receptors in circular colonic muscle which were unaffected either by selective concentrations of methysergide or tetrodotoxin.
|
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] |
PMID:21258
|
Influence of pyridylisatogen tosylate on contractions produced by ATP and by purinergic stimulation in the terminal ileum of the guinea-pig.
|
2-2'Pyridylisatogen tosylate (PIT), which antagonizes the inhibitory action of ATP in the taenia caeci, did not antagonize the excitatory effects of exogenous ATP and of purinergic stimulation of the terminal guinea-pig ileum. PIT (0-5--2-5 muM) potentiated the ATP-induced contractions and also the contractions produced by potassium chloride, though the potentiation could not be related to the dose in every experiment. The responses to noradrenaline, adrenaline and histamine were slightly inhibited. PIT also potentiated the contractions produced by electrical stimulation of intramural purinergic nerves when either an alternate or uniform stimulation pattern was used. The present results in which the preparation is contracted by ATP are opposite to those obtained with PIT on the taenia caeci, which is relaxed by ATP. This raises a question of duality or plurality of receptors for ATP.
|
Influence of pyridylisatogen tosylate on contractions produced by ATP and by purinergic stimulation in the terminal ileum of the guinea-pig. 2-2'Pyridylisatogen tosylate (PIT), which antagonizes the inhibitory action of ATP in the taenia caeci, did not antagonize the excitatory effects of exogenous ATP and of purinergic stimulation of the terminal guinea-pig ileum. PIT (0-5--2-5 muM) potentiated the ATP-induced contractions and also the contractions produced by potassium chloride, though the potentiation could not be related to the dose in every experiment. The responses to noradrenaline, adrenaline and histamine were slightly inhibited. PIT also potentiated the contractions produced by electrical stimulation of intramural purinergic nerves when either an alternate or uniform stimulation pattern was used. The present results in which the preparation is contracted by ATP are opposite to those obtained with PIT on the taenia caeci, which is relaxed by ATP. This raises a question of duality or plurality of receptors for ATP.
|
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] |
PMID:21259
|
Effect of two non tricyclic antidepressant drugs on [14C]5-hydroxytryptamine uptake by rat platelets.
|
The uptake of 14C-5-HT by rat blood platelets was examined in vitro in experimental conditions which allowed measurement of the initial velocity and excluded other passive processes across the cell membrane. In these conditions, the effect of two non tricyclic antidepressant drugs (Lilly 110140 and trazodone) was investigated. Lilly 110140 was as active as chlorimipramine and several times more active than imipramine as an inhibitor of 14C-5-HT uptake. Like chlorimipramine, Lilly 110140 appeared to be either a non-competitive or an uncompetitive inhibitor, according to the concentration of drug used. Trazodone also inhibited 14C-5-HT uptake by platelets but to a lesser extent than chlorimipramine, imipramine or Lilly 110140. m-Chlorophenylpiperazine, a possible metabolite of trazodone, was about 3 times more potent an inhibitor than the parent molecule. Both compounds acted non-competitively. Compared with published data on the effect of Lilly 110140 and trazodone on brain 5-HT, the present results support the suggestion that rat platelets are a useful pharmacological model of serotoninergic nerve endings.
|
Effect of two non tricyclic antidepressant drugs on [14C]5-hydroxytryptamine uptake by rat platelets. The uptake of 14C-5-HT by rat blood platelets was examined in vitro in experimental conditions which allowed measurement of the initial velocity and excluded other passive processes across the cell membrane. In these conditions, the effect of two non tricyclic antidepressant drugs (Lilly 110140 and trazodone) was investigated. Lilly 110140 was as active as chlorimipramine and several times more active than imipramine as an inhibitor of 14C-5-HT uptake. Like chlorimipramine, Lilly 110140 appeared to be either a non-competitive or an uncompetitive inhibitor, according to the concentration of drug used. Trazodone also inhibited 14C-5-HT uptake by platelets but to a lesser extent than chlorimipramine, imipramine or Lilly 110140. m-Chlorophenylpiperazine, a possible metabolite of trazodone, was about 3 times more potent an inhibitor than the parent molecule. Both compounds acted non-competitively. Compared with published data on the effect of Lilly 110140 and trazodone on brain 5-HT, the present results support the suggestion that rat platelets are a useful pharmacological model of serotoninergic nerve endings.
|
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] |
PMID:21260
|
Analysis of the beta-receptor mediated effect on slow-contracting skeletal muscle in vitro.
|
Subtetanic contractions of the guinea-pig isolated soleus, a slow-contracting skeletal muscle, were evoked by transmural field-stimulation. Isoprenaline caused a dose-dependent depression of the contractions. This effect was inhibited by propranolol and H 35/25 (1-(p-tolyl-2-isopropylamino-1-propanol) but not by practolol. Similar results were obtained for terbutaline. Tazolol and H 80/62 (1-isopropylamino-3-(p-hydroxyphenoxy)-2-propanol (HCl), selective beta1-agonists, had no effect per se but inhibited the effect of terbutaline. Adrenaline, noradrenaline, and dopamine all caused a dose-dependent decrease in the force of the soleus contractions, their potencies being in that order. Tyramine did not appreciably affect the contractions nor did it inhibit the effect of terbutaline. Pretreatment with reserpine, if anything, increased the response to terbutaline. It is concluded, in conformity with previous in vivo studies, that the adrenergic receptor mediating the effect on the soleus muscle contractions is of the beta2-type. Indirect sympathomimetic effects do not contribute to the responses observed on the isolated soleus muscle.
|
Analysis of the beta-receptor mediated effect on slow-contracting skeletal muscle in vitro. Subtetanic contractions of the guinea-pig isolated soleus, a slow-contracting skeletal muscle, were evoked by transmural field-stimulation. Isoprenaline caused a dose-dependent depression of the contractions. This effect was inhibited by propranolol and H 35/25 (1-(p-tolyl-2-isopropylamino-1-propanol) but not by practolol. Similar results were obtained for terbutaline. Tazolol and H 80/62 (1-isopropylamino-3-(p-hydroxyphenoxy)-2-propanol (HCl), selective beta1-agonists, had no effect per se but inhibited the effect of terbutaline. Adrenaline, noradrenaline, and dopamine all caused a dose-dependent decrease in the force of the soleus contractions, their potencies being in that order. Tyramine did not appreciably affect the contractions nor did it inhibit the effect of terbutaline. Pretreatment with reserpine, if anything, increased the response to terbutaline. It is concluded, in conformity with previous in vivo studies, that the adrenergic receptor mediating the effect on the soleus muscle contractions is of the beta2-type. Indirect sympathomimetic effects do not contribute to the responses observed on the isolated soleus muscle.
|
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] |
PMID:21261
|
Biochemical and pharmacological studies on amineptine (S 1694) and (+)-amphetamine in the rat.
|
The pharmacological activities of amineptine (S 1694) and (+)-amphetamine and their interaction with biogenic amines have been examined in rats. The locomotor activity, stereotyped behaviour and hypothermia induced by amineptine were similar to but not as marked as those produced by (+)-amphetamine, and there was little or no anorectic action. Amineptine does not modify the concentrations of brain noradrenaline or acetylcholine which are respectively reduced and increased by (+)-amphetamine. Moreover, amineptine does not affect significantly the decrease of brain noradrenaline induced by an intraventricular injection of 6-hydroxydopamine, an effect significantly antagonized by (+)-amphetamine. On the other hand, like amphetamine, amineptine significantly reduces the effect of 6-hydroxy-dopamine on brain dopamine. Both drugs increase the striatal concentrations of homovanillic acid and show a cross tolerance in this action. Therefore they could act similarly on the striatal dopaminergine system. Amineptine thus appears to be a new type of antidepressant with a brain biochemical profile differing from that of other drugs used in depressive disorders.
|
Biochemical and pharmacological studies on amineptine (S 1694) and (+)-amphetamine in the rat. The pharmacological activities of amineptine (S 1694) and (+)-amphetamine and their interaction with biogenic amines have been examined in rats. The locomotor activity, stereotyped behaviour and hypothermia induced by amineptine were similar to but not as marked as those produced by (+)-amphetamine, and there was little or no anorectic action. Amineptine does not modify the concentrations of brain noradrenaline or acetylcholine which are respectively reduced and increased by (+)-amphetamine. Moreover, amineptine does not affect significantly the decrease of brain noradrenaline induced by an intraventricular injection of 6-hydroxydopamine, an effect significantly antagonized by (+)-amphetamine. On the other hand, like amphetamine, amineptine significantly reduces the effect of 6-hydroxy-dopamine on brain dopamine. Both drugs increase the striatal concentrations of homovanillic acid and show a cross tolerance in this action. Therefore they could act similarly on the striatal dopaminergine system. Amineptine thus appears to be a new type of antidepressant with a brain biochemical profile differing from that of other drugs used in depressive disorders.
|
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] |
PMID:21278
|
pH-stat titration of aluminum hydroxide gel.
|
The pH-stat titration of aluminum hydroxide gel was evaluated and was affected by pH, temperature, concentration, and ionic strength. Control of these parameters resulted in a highly sensitive and reproducible in vitro antacid test. The utility of the pH-stat test was illustrated by monitoring the aging of several carbonate-containing aluminum hydroxide gels and by comparing the antacid properties as measured by the pH-stat titration, the acid-consuming capacity, the Rossett-Rice test, and the test proposed by the food and Drug Administration Drug Evaluation Panel. The pH-stat titration also was useful for relatively nonreactive aluminum hydroxide gels. The use of sodium fluoride as the reaction medium extended the capability of the pH-stat titration to monitor the aging of chloride-containing gels. The pH-stat titrigram was interpreted in terms of a previously published polymer model of the structure of a chloride-containing aluminum hydroxide gel. The acid reactivity of relatively nonreactive gel is believed to be due totally to the chemical neutralization of acid, because the milliequivalents of aluminum ion appearing in solution is the same as the milliequivalents of acid neutralized throughout the ph-stat titration.
|
pH-stat titration of aluminum hydroxide gel. The pH-stat titration of aluminum hydroxide gel was evaluated and was affected by pH, temperature, concentration, and ionic strength. Control of these parameters resulted in a highly sensitive and reproducible in vitro antacid test. The utility of the pH-stat test was illustrated by monitoring the aging of several carbonate-containing aluminum hydroxide gels and by comparing the antacid properties as measured by the pH-stat titration, the acid-consuming capacity, the Rossett-Rice test, and the test proposed by the food and Drug Administration Drug Evaluation Panel. The pH-stat titration also was useful for relatively nonreactive aluminum hydroxide gels. The use of sodium fluoride as the reaction medium extended the capability of the pH-stat titration to monitor the aging of chloride-containing gels. The pH-stat titrigram was interpreted in terms of a previously published polymer model of the structure of a chloride-containing aluminum hydroxide gel. The acid reactivity of relatively nonreactive gel is believed to be due totally to the chemical neutralization of acid, because the milliequivalents of aluminum ion appearing in solution is the same as the milliequivalents of acid neutralized throughout the ph-stat titration.
|
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] |
PMID:21279
|
Relationship between zero point of charge and solubility product for hydroxides of polyvalent cations.
|
The zero point of charge (ZPC) of slightly soluble compounds is the pH at which their particles suspended in water have zero charge. The ZPC values of slightly soluble hydroxides were compared with their solubility product in the form of its negative logarithm, pKSP, and with th pH of their suspensions in pure water, pHSP, which is a function of pKSP. The ZPC-pKSP relation was nonlinear while the ZPC-pHSP relation was linear. Either equation can used to estimate the ZPC value of a hydroxide from its solubility product. The ZPC of a given hydroxide was higher than its pHSP because polyvalent cations are more extensively adsorbed and less extensively desorbed from the particle surface than the monovalent hydroxide ion. At the pHSP, there are equivalent amounts of the cation and of the hydroxide anion in solution, but the surface layer of the hydroxide particle contains an excess cation on an equivalent basis. This imbalance confers a positive charge to the particle. The solubility product of aluminum hydroxide, redetermined at 25 degrees by means of pH measurements, was 8 X 10(-33). Its ZPC, redetermined by microelectrophoresis, was 8.5 +/- 0.1.
|
Relationship between zero point of charge and solubility product for hydroxides of polyvalent cations. The zero point of charge (ZPC) of slightly soluble compounds is the pH at which their particles suspended in water have zero charge. The ZPC values of slightly soluble hydroxides were compared with their solubility product in the form of its negative logarithm, pKSP, and with th pH of their suspensions in pure water, pHSP, which is a function of pKSP. The ZPC-pKSP relation was nonlinear while the ZPC-pHSP relation was linear. Either equation can used to estimate the ZPC value of a hydroxide from its solubility product. The ZPC of a given hydroxide was higher than its pHSP because polyvalent cations are more extensively adsorbed and less extensively desorbed from the particle surface than the monovalent hydroxide ion. At the pHSP, there are equivalent amounts of the cation and of the hydroxide anion in solution, but the surface layer of the hydroxide particle contains an excess cation on an equivalent basis. This imbalance confers a positive charge to the particle. The solubility product of aluminum hydroxide, redetermined at 25 degrees by means of pH measurements, was 8 X 10(-33). Its ZPC, redetermined by microelectrophoresis, was 8.5 +/- 0.1.
|
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] |
PMID:21280
|
In vitro photodecomposition of uric acid in presence of riboflavin II.
|
In vitro studies on the photodecomposition of uric acid in the presence of the monosodium salt of riboflavin 5'-phosphate in buffers at various pH values, in methanol, and in human plasma are reported. The decomposition rate increased with increasing pH and was independent of solvent or buffer species. The mechanism appears to be an energy transfer process involving triplet riboflavin and single oxygen. Riboflavin-enhanced photodecomposition of uric acid occurred in vitro in hyperuricemic human plasma.
|
In vitro photodecomposition of uric acid in presence of riboflavin II. In vitro studies on the photodecomposition of uric acid in the presence of the monosodium salt of riboflavin 5'-phosphate in buffers at various pH values, in methanol, and in human plasma are reported. The decomposition rate increased with increasing pH and was independent of solvent or buffer species. The mechanism appears to be an energy transfer process involving triplet riboflavin and single oxygen. Riboflavin-enhanced photodecomposition of uric acid occurred in vitro in hyperuricemic human plasma.
|
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] |
PMID:21281
|
Effects of adenine nucleotides on oxidation of phenothiazine tranquilizers.
|
The effects of adenosine diphosphate and triphosphate on the periodic acid oxidation of the phenothiazine tranquilizing drugs were studied. The principal effect was a marked reduction in the rate of formation and decay of the drug free radical. The oxidation rates of the nucleotide free drugs seemed to be most strongly influenced by the inductive effects of substituents at the 2-position of the phenothiazine nucleus. However, the oxidation rates of the drugs in the presence of nucleotide were most strongly influenced by the substituents at the 10-position. Variations of the structure of substituents at the 10-position have only a modest effect on the electronic state of the phenothiazine nucleus. Therefore, the marked effect of structural variation in the 10-substituents in the presence of nucleotide on the periodate oxidation rate most likely is an expression of steric effects related to an interaction between drug and nucleotide.
|
Effects of adenine nucleotides on oxidation of phenothiazine tranquilizers. The effects of adenosine diphosphate and triphosphate on the periodic acid oxidation of the phenothiazine tranquilizing drugs were studied. The principal effect was a marked reduction in the rate of formation and decay of the drug free radical. The oxidation rates of the nucleotide free drugs seemed to be most strongly influenced by the inductive effects of substituents at the 2-position of the phenothiazine nucleus. However, the oxidation rates of the drugs in the presence of nucleotide were most strongly influenced by the substituents at the 10-position. Variations of the structure of substituents at the 10-position have only a modest effect on the electronic state of the phenothiazine nucleus. Therefore, the marked effect of structural variation in the 10-substituents in the presence of nucleotide on the periodate oxidation rate most likely is an expression of steric effects related to an interaction between drug and nucleotide.
|
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] |
PMID:21282
|
Stability of prostaglandin E1 and dinoprostone (prostaglandin E2) under strongly acidic and basic conditions.
|
The stability of prostaglandin E1 and dinoprostone was investigated at the extremes of the pH range (less than or equal to 3 and greater than or equal to 10) in the sequence prostaglandin E leads to prostaglandin A leads to prostaglandin B. The degradation rate is first order with hydrogen-ion and hydroxide-ion concentrations. Separation and analysis of the E prostaglandins were accomplished by TLC and UV spectrophotometry. At the lowest pH values and at elevated or low temperatures, significant amounts of 15-epiprostaglandin E were present. Apparent activation energies for the total dinoprostone loss, calculated from elevated temperature data, were 21 kcal/mole in the strongly acidic region and about 18 kcal/mole at pH 3. Corresponding studies in the alkaline region led to a derived arrhenius activation energy of 15 kcal/mole with the appearance of significant amounts of 8-isoprostaglandin E. This difference in activation energies may reflect the different mechanisms operant at high and low pH values.
|
Stability of prostaglandin E1 and dinoprostone (prostaglandin E2) under strongly acidic and basic conditions. The stability of prostaglandin E1 and dinoprostone was investigated at the extremes of the pH range (less than or equal to 3 and greater than or equal to 10) in the sequence prostaglandin E leads to prostaglandin A leads to prostaglandin B. The degradation rate is first order with hydrogen-ion and hydroxide-ion concentrations. Separation and analysis of the E prostaglandins were accomplished by TLC and UV spectrophotometry. At the lowest pH values and at elevated or low temperatures, significant amounts of 15-epiprostaglandin E were present. Apparent activation energies for the total dinoprostone loss, calculated from elevated temperature data, were 21 kcal/mole in the strongly acidic region and about 18 kcal/mole at pH 3. Corresponding studies in the alkaline region led to a derived arrhenius activation energy of 15 kcal/mole with the appearance of significant amounts of 8-isoprostaglandin E. This difference in activation energies may reflect the different mechanisms operant at high and low pH values.
|
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] |
PMID:21283
|
Tetrazole analogs of phenylalanine derivatives as tyrosine hydroxylase inhibitors.
|
Eight new tetrazole analogs of phenylalanine derivatives in which the carboxyl group was replaced by a tetrazole ring were synthesized. At a concentration of 2.5 time 10(-5) M, each compound exhibited greater than 50% inhibition of tyrosine hydroxylase activity.
|
Tetrazole analogs of phenylalanine derivatives as tyrosine hydroxylase inhibitors. Eight new tetrazole analogs of phenylalanine derivatives in which the carboxyl group was replaced by a tetrazole ring were synthesized. At a concentration of 2.5 time 10(-5) M, each compound exhibited greater than 50% inhibition of tyrosine hydroxylase activity.
|
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] |
PMID:21284
|
Kinetics of concomitant degradation of tetracycline to epitetracycline, anhydrotetracycline, and epianhydrotetracycline in acid phosphate solution.
|
The concentrations of tetracycline, epitetracycline, anhydrotetracycline, and epianhydrotetracycline in pH 1.5 phosphate solution were followed as a function of time at four temperatures. Separation and quantification of all four species were accomplished using high-pressure liquid chromatography. Through nonlinear regression analysis, rate constants for the reversible first-order epimerization of tetracycline and anhydrotetracycline and for the first-order dehydration of tetracycline and epitetracycline were obtained. Solutions to the differential equations obtained through Laplace transforms successfully predict concentrations found experimentally. The energy of activation for each reaction step was calculated and ranged from 15 to 27 kcal/mole. The rate constants for tetracycline and epitetracycline dehydration conform with those of earlier studies that used different experimental methods. The study shows that epimerization of tetracycline and anhydrotetracycline can take place at a low pH.
|
Kinetics of concomitant degradation of tetracycline to epitetracycline, anhydrotetracycline, and epianhydrotetracycline in acid phosphate solution. The concentrations of tetracycline, epitetracycline, anhydrotetracycline, and epianhydrotetracycline in pH 1.5 phosphate solution were followed as a function of time at four temperatures. Separation and quantification of all four species were accomplished using high-pressure liquid chromatography. Through nonlinear regression analysis, rate constants for the reversible first-order epimerization of tetracycline and anhydrotetracycline and for the first-order dehydration of tetracycline and epitetracycline were obtained. Solutions to the differential equations obtained through Laplace transforms successfully predict concentrations found experimentally. The energy of activation for each reaction step was calculated and ranged from 15 to 27 kcal/mole. The rate constants for tetracycline and epitetracycline dehydration conform with those of earlier studies that used different experimental methods. The study shows that epimerization of tetracycline and anhydrotetracycline can take place at a low pH.
|
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] |
PMID:21285
|
Evidence for antral inhibition of pentagastrin from experiments using mucosal cooling.
|
1. The acid secretion of the fundic mucosa in Heidenhain pouches in response to pentagastrin became progressively less as the pouch mucosa was cooled. 2. When a cooled Heidenhain pouch in an animal receiving pentagastrin was warmed, acid and pepsin secretion from the main stomach was depressed. Change from warm to cool produced no obvious effect. 3. In animals receiving pentagastrin continuously, but not in those receiving histamine, lowering the temperature in an antral pouch, or the application of local anaesthetics to its mucosa, increased acid and pepsin secretion from the main stomach when the antral pouch was fully innervated. 4. This effect could readily be abolished by ganglionic and beta-adrenergic blockade, but not by bilateral vagal block in the neck, thus suggesting a sympathetically mediated inhibitory mechanism of pyloric origin. 5. The effect of indirect vagal stimulation, using 2-deoxy-D-glucose on secretion from the main stomach, was augmented by pyloric antral local anaesthesia and depressed by antral cooling.
|
Evidence for antral inhibition of pentagastrin from experiments using mucosal cooling. 1. The acid secretion of the fundic mucosa in Heidenhain pouches in response to pentagastrin became progressively less as the pouch mucosa was cooled. 2. When a cooled Heidenhain pouch in an animal receiving pentagastrin was warmed, acid and pepsin secretion from the main stomach was depressed. Change from warm to cool produced no obvious effect. 3. In animals receiving pentagastrin continuously, but not in those receiving histamine, lowering the temperature in an antral pouch, or the application of local anaesthetics to its mucosa, increased acid and pepsin secretion from the main stomach when the antral pouch was fully innervated. 4. This effect could readily be abolished by ganglionic and beta-adrenergic blockade, but not by bilateral vagal block in the neck, thus suggesting a sympathetically mediated inhibitory mechanism of pyloric origin. 5. The effect of indirect vagal stimulation, using 2-deoxy-D-glucose on secretion from the main stomach, was augmented by pyloric antral local anaesthesia and depressed by antral cooling.
|
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] |
PMID:21286
|
Effects of neurochemicals upon a dinoflagellate photoresponse.
|
Photoresponsiveness by Gymnodinium splendens Lebour was monitored quantitatively by a microscope-television system. Exposure to the catecholamines DOPA and Dopamine caused a decrease in light sensitivity, while 0.01 mM norepinephine, or isoproterenol did not affect photoresponsiveness. Classical catecholamine blocking agents, dichloroisoproterenol, propranolol, and dibenzyline, and an inhibitor of DOPA synthesis, alpha-methyl-rho-tyrosine, caused an increase in sensitivity. In addition, acetylcholine and an inhibitor of acetylcholinesterase activity, eserine, caused an increase in sensitivity, while an inhibitor of acetylcholine action atropine, had the opposite effect. These experiments suggest that G. splendens may have an antagonistic catecholamine-cholinergic system which participates in regulating photosensitivity.
|
Effects of neurochemicals upon a dinoflagellate photoresponse. Photoresponsiveness by Gymnodinium splendens Lebour was monitored quantitatively by a microscope-television system. Exposure to the catecholamines DOPA and Dopamine caused a decrease in light sensitivity, while 0.01 mM norepinephine, or isoproterenol did not affect photoresponsiveness. Classical catecholamine blocking agents, dichloroisoproterenol, propranolol, and dibenzyline, and an inhibitor of DOPA synthesis, alpha-methyl-rho-tyrosine, caused an increase in sensitivity. In addition, acetylcholine and an inhibitor of acetylcholinesterase activity, eserine, caused an increase in sensitivity, while an inhibitor of acetylcholine action atropine, had the opposite effect. These experiments suggest that G. splendens may have an antagonistic catecholamine-cholinergic system which participates in regulating photosensitivity.
|
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] |
PMID:21287
|
Toxoplasma gondii-vertebrate cell interactions. I. The influence of bicarbonate ion, CO2, pH and host cell culture age on the invasion of vertebrate cells in vitro.
|
A controlled-environment culture system was used to show that both physical and biologic parameters can influence the penetration of vertebrate cells by Toxoplasma gondii. The optimum bicarbonate ion concentration for the penetration of bovine embryo skeletal muscle (BESM) cells is 36.25 mM. Higher or lower bicarbonate ion concentrations are increasingly inhibitory to penetration. As CO2 increases in the range from 0.5-3.7 mM, penetration is progressively inhibited. No relationship was found between penetration and pH in the pH range of 6.949-7.765. The culture age of the BESM cells directly influenced the ability of the parasites to penetrate the cells. Older BESM cells were more refractory to penetration than younger cells.
|
Toxoplasma gondii-vertebrate cell interactions. I. The influence of bicarbonate ion, CO2, pH and host cell culture age on the invasion of vertebrate cells in vitro. A controlled-environment culture system was used to show that both physical and biologic parameters can influence the penetration of vertebrate cells by Toxoplasma gondii. The optimum bicarbonate ion concentration for the penetration of bovine embryo skeletal muscle (BESM) cells is 36.25 mM. Higher or lower bicarbonate ion concentrations are increasingly inhibitory to penetration. As CO2 increases in the range from 0.5-3.7 mM, penetration is progressively inhibited. No relationship was found between penetration and pH in the pH range of 6.949-7.765. The culture age of the BESM cells directly influenced the ability of the parasites to penetrate the cells. Older BESM cells were more refractory to penetration than younger cells.
|
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] |
PMID:21288
|
Specific labeling of intracellular Toxoplasma gondii with uracil.
|
Radioactive uracil was not significantly incorporated into the nucleic acids of human fibroblast cells. Infection of these cells with Toxoplasma gondii resulted in an exponential increase in the rate of uracil incorporation that paralleled the exponential growth of the parasite. One day after infection the rate of uracil incorporation was increased 100-fold. It was established by autoradiography that all of the [3H] uracil was incorporated into the intracellular parasites. A possible explanation for this difference in ability to use uracil is our observation that the specific activity of uridine phosphorylase was 100-fold greater in partially purified parasites than in the host cell.
|
Specific labeling of intracellular Toxoplasma gondii with uracil. Radioactive uracil was not significantly incorporated into the nucleic acids of human fibroblast cells. Infection of these cells with Toxoplasma gondii resulted in an exponential increase in the rate of uracil incorporation that paralleled the exponential growth of the parasite. One day after infection the rate of uracil incorporation was increased 100-fold. It was established by autoradiography that all of the [3H] uracil was incorporated into the intracellular parasites. A possible explanation for this difference in ability to use uracil is our observation that the specific activity of uridine phosphorylase was 100-fold greater in partially purified parasites than in the host cell.
|
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] |
PMID:21289
|
Monoamine oxidase and catechol-O-methyl transferase activity in Tetrahymena.
|
Tetrahymena pyriformis strain HSM was found to have monomine oxidase (MAO) and a catechol-3-methyl transferase-like (COMT) activity. As in mammalian tissues, the MAO activity is predominantly localized in the mitochondrial pellet and COMT in the cytosol. The COMT-like activity was present in amounts comparable to several mouse tissues and was inhibited by tropolone. MAO activity was much lower than in any of the mouse tissues tested, and its activity varied greatly from preparation to preparation. The substrate preference of Tetrahymena MAO was tryptamine greater than serotonin greater than dopamine, and activity increased with increasing pH from pH 6.5 to pH 7.8, as does that of mouse liver MAO. Teh Km of Tetrahymena MAO for tryptamine was approximately 4 micrometer, an order of magnitude lower than that of mouse liver MAO. Sensitivity of inhibition by MAO inhibitors was variable. In some preparations, no inhibition was observed. In others clear inhibition was obtained, harmine and clorgyline being among the most potent inhibitors.
|
Monoamine oxidase and catechol-O-methyl transferase activity in Tetrahymena. Tetrahymena pyriformis strain HSM was found to have monomine oxidase (MAO) and a catechol-3-methyl transferase-like (COMT) activity. As in mammalian tissues, the MAO activity is predominantly localized in the mitochondrial pellet and COMT in the cytosol. The COMT-like activity was present in amounts comparable to several mouse tissues and was inhibited by tropolone. MAO activity was much lower than in any of the mouse tissues tested, and its activity varied greatly from preparation to preparation. The substrate preference of Tetrahymena MAO was tryptamine greater than serotonin greater than dopamine, and activity increased with increasing pH from pH 6.5 to pH 7.8, as does that of mouse liver MAO. Teh Km of Tetrahymena MAO for tryptamine was approximately 4 micrometer, an order of magnitude lower than that of mouse liver MAO. Sensitivity of inhibition by MAO inhibitors was variable. In some preparations, no inhibition was observed. In others clear inhibition was obtained, harmine and clorgyline being among the most potent inhibitors.
|
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] |
PMID:21290
|
Poly(ethylene oxide), a new slowing agent for protozoa.
|
The water-soluble, viscoelastic resin Polyox WSR 301), a poly(ethylene oxide) of high molecular weight (approximately 4 million) is introduces as a new slowing agent for protozoa. Generally, as the kinetic viscosity of the resin increased from 0.25% to 1% (w/v), the swimming velocity of Euglena gracilis, Didnium nasutum, Paramecium aurelia, Blepharisma undulans, and Prorodon platyodon decreased. The 1.0% solution had the highest viscosity and decreased velocity more effectively than 1.0% methyl cellulose and Protoslo solutions. The Polyox solutions differed from those of methyl cellulose and Protoslo by having, in addition to viscous drag, an elastic recoil that pulled the protozoa backwards when their swimming efforts stopped. The toxicity of these slowing agents was determined using 10 P. aurelia/test slide preparation. Paramecium numbers decreased in 1.0% methyl cellulose and Protoslo to nearly zero by 24 hr; in Polyox, not only were most these ciliates alive after 24 hr, but many survived for 96 hr and divisions occurred in 0.25% and 0.50% solutions.
|
Poly(ethylene oxide), a new slowing agent for protozoa. The water-soluble, viscoelastic resin Polyox WSR 301), a poly(ethylene oxide) of high molecular weight (approximately 4 million) is introduces as a new slowing agent for protozoa. Generally, as the kinetic viscosity of the resin increased from 0.25% to 1% (w/v), the swimming velocity of Euglena gracilis, Didnium nasutum, Paramecium aurelia, Blepharisma undulans, and Prorodon platyodon decreased. The 1.0% solution had the highest viscosity and decreased velocity more effectively than 1.0% methyl cellulose and Protoslo solutions. The Polyox solutions differed from those of methyl cellulose and Protoslo by having, in addition to viscous drag, an elastic recoil that pulled the protozoa backwards when their swimming efforts stopped. The toxicity of these slowing agents was determined using 10 P. aurelia/test slide preparation. Paramecium numbers decreased in 1.0% methyl cellulose and Protoslo to nearly zero by 24 hr; in Polyox, not only were most these ciliates alive after 24 hr, but many survived for 96 hr and divisions occurred in 0.25% and 0.50% solutions.
|
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] |
PMID:21291
|
Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans.
|
A series of N-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans was synthesized and evaluated for their narcotic analgesic and antagonistic activities. Compounds 2a and 22 were as potent as morphine in the writhing (PPQ) and hot-plate tests, while a number of compounds demonstrated antagonistic activities greater than nalorphine. Generally, the compounds in this series show activities somewhat greater than the comparable compounds in the 5,9alpha-dimethyl-6,7-benzomorphan series for analgesic effect and similar or slightly less antagonistic potency.
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Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans. A series of N-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans was synthesized and evaluated for their narcotic analgesic and antagonistic activities. Compounds 2a and 22 were as potent as morphine in the writhing (PPQ) and hot-plate tests, while a number of compounds demonstrated antagonistic activities greater than nalorphine. Generally, the compounds in this series show activities somewhat greater than the comparable compounds in the 5,9alpha-dimethyl-6,7-benzomorphan series for analgesic effect and similar or slightly less antagonistic potency.
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] |
PMID:21292
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Application of the Free-Wilson technique to structurally related series of homologues. Quantitative structure-activity relationship studies of narcotic analgetics.
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A series of benzomorphans with ED50 values determined in vivo by the hot-plate method in mice is analyzed by the modified Free-Wilson method. The QSAR yields 36 substituent constants (ai) with contributions to the overall activity in agreement with experimental data. Substituent constant values obtained for benzomorphans are used in calculating log (1/C) values for six morphinans. An excellent correlation is obtained (r = 0.95) between the six calculated and observed activities. The possibility of extending the Free-Wilson approach from one series of homologues to another is demonstrated.
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Application of the Free-Wilson technique to structurally related series of homologues. Quantitative structure-activity relationship studies of narcotic analgetics. A series of benzomorphans with ED50 values determined in vivo by the hot-plate method in mice is analyzed by the modified Free-Wilson method. The QSAR yields 36 substituent constants (ai) with contributions to the overall activity in agreement with experimental data. Substituent constant values obtained for benzomorphans are used in calculating log (1/C) values for six morphinans. An excellent correlation is obtained (r = 0.95) between the six calculated and observed activities. The possibility of extending the Free-Wilson approach from one series of homologues to another is demonstrated.
|
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] |
PMID:21293
|
Synthesis of 1-substituted analogues of trimetoquinol possessing differential and selective beta-adrenergic properties.
|
The synthesis of the 1,1-disubstituted tetrahydroisoquinoline analogues, 1-methyl-1-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (2) and 1-benzyl-1-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3), is described. The profile of beta-adrenergic activity for these analogues was determined and compared to that of trimetoquinol (1) in isolated guinea pig atrial, tracheal, and rat adipocyte preparations. Unexpected selective beta1-blocking activity in guinea pig trachea was noted with analogue 3. With the exception of 2 in guinea pig atria, 2 and 3 did not possess any beta-stimulant activity. Substitution at the 1 position of trimetoquinol (1) has revealed qualitative differences in beta-adrenergic activity.
|
Synthesis of 1-substituted analogues of trimetoquinol possessing differential and selective beta-adrenergic properties. The synthesis of the 1,1-disubstituted tetrahydroisoquinoline analogues, 1-methyl-1-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (2) and 1-benzyl-1-(3,4,5-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3), is described. The profile of beta-adrenergic activity for these analogues was determined and compared to that of trimetoquinol (1) in isolated guinea pig atrial, tracheal, and rat adipocyte preparations. Unexpected selective beta1-blocking activity in guinea pig trachea was noted with analogue 3. With the exception of 2 in guinea pig atria, 2 and 3 did not possess any beta-stimulant activity. Substitution at the 1 position of trimetoquinol (1) has revealed qualitative differences in beta-adrenergic activity.
|
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] |
PMID:21294
|
A systematic and comprehensive approach to teaching and evaluating interpersonal skills.
|
This study addressed one problem with current methods for teaching and evaluating interpersonal skills: the failure to include a wide range of behaviors reported in the literature as contributing to patient dissatisfaction and noncompliance. To address this concern, the authors developed a comprehensive interpersonal skills training program and a pretest-posttest evaluation. The tests were administered to two student groups one of which received the interpersonal skills instruction. The student group exposed to the training exhibited a significant positive change from pretest to posttest. Additionally the change for this group was significantly greater than the change for the group not exposed to interpersonal skills instruction.
|
A systematic and comprehensive approach to teaching and evaluating interpersonal skills. This study addressed one problem with current methods for teaching and evaluating interpersonal skills: the failure to include a wide range of behaviors reported in the literature as contributing to patient dissatisfaction and noncompliance. To address this concern, the authors developed a comprehensive interpersonal skills training program and a pretest-posttest evaluation. The tests were administered to two student groups one of which received the interpersonal skills instruction. The student group exposed to the training exhibited a significant positive change from pretest to posttest. Additionally the change for this group was significantly greater than the change for the group not exposed to interpersonal skills instruction.
|
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] |
PMID:21295
|
The effect of certain rater roles on confidence in physician's assistant ratings.
|
Previous research on the psychology of confidence suggests that the more confident a rater is in his judgment the more accurate is his rating. The purpose of the present study was to investigate possible differences among raters in their confidence in competency ratings which they had provided. Results indicated significant differences due to the rater's interpersonal role with the ratee and the particular aspect of competence rated. Greater simple structure of competence ratings when adjusted for rater confidence is also shown. Rater confidence is discussed as an index for rater selection and as a moderator variable for competence ratings.
|
The effect of certain rater roles on confidence in physician's assistant ratings. Previous research on the psychology of confidence suggests that the more confident a rater is in his judgment the more accurate is his rating. The purpose of the present study was to investigate possible differences among raters in their confidence in competency ratings which they had provided. Results indicated significant differences due to the rater's interpersonal role with the ratee and the particular aspect of competence rated. Greater simple structure of competence ratings when adjusted for rater confidence is also shown. Rater confidence is discussed as an index for rater selection and as a moderator variable for competence ratings.
|
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] |
PMID:21297
|
Normal acid-base status of arterial blood from the conscious, chair-restrained squirrel monkey.
|
Normal acid-base status of arterial blood (pHa =7.40, PaCO2=38.1 Torr) was demonstrated for conscious, restrained squirrel monkeys when environmental stimuli were minimized and monkeys are habituated to experimental procedures. These results indicate the potential for using squirrel monkeys in experiments in which normal acid-base status is a significant factor.
|
Normal acid-base status of arterial blood from the conscious, chair-restrained squirrel monkey. Normal acid-base status of arterial blood (pHa =7.40, PaCO2=38.1 Torr) was demonstrated for conscious, restrained squirrel monkeys when environmental stimuli were minimized and monkeys are habituated to experimental procedures. These results indicate the potential for using squirrel monkeys in experiments in which normal acid-base status is a significant factor.
|
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] |
PMID:21298
|
Multifocal candidiasis in a capuchin monkey (Cebus apella).
|
Candidiasis involving nasal, pharyngeal, and intestinal mucosal surfaces and a pharyngeal lymph node was demonstrated microscopically in a young adult female capuchin monkey (Cebus apella) experimentally infected with Schistosoma haematobium (Iran strain). Persistent nasal exudation and weight loss characterized the clinical disease preceding the animal's death.
|
Multifocal candidiasis in a capuchin monkey (Cebus apella). Candidiasis involving nasal, pharyngeal, and intestinal mucosal surfaces and a pharyngeal lymph node was demonstrated microscopically in a young adult female capuchin monkey (Cebus apella) experimentally infected with Schistosoma haematobium (Iran strain). Persistent nasal exudation and weight loss characterized the clinical disease preceding the animal's death.
|
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] |
PMID:21301
|
Management of dental trauma in children and adolescents.
|
The emergency treatment of dental trauma has traditionally been handled in the emergency rooms of medical centers, or in the dental office. With increasing emphasis on comprehensive medical care, and the tendency of more recent graduates to locate in rural areas, there is a growing trend for physicians to be involved in providing emergency care for traumatic injuries to the dental and oral tissues. The authors discuss the etiology of dental trauma and the highly psychologic impact of such injuries upon the patient and parents. Techniques for prevention and a comprehensive plan are outlined for systematic history taking and examination. A classification of eight levels of dental injuries (5), techniques for the emergency, and subsequent restorative care are given. Emphasis is placed upon immediate care which can, if necessary, be provided by the physician pending referral to a dentist.
|
Management of dental trauma in children and adolescents. The emergency treatment of dental trauma has traditionally been handled in the emergency rooms of medical centers, or in the dental office. With increasing emphasis on comprehensive medical care, and the tendency of more recent graduates to locate in rural areas, there is a growing trend for physicians to be involved in providing emergency care for traumatic injuries to the dental and oral tissues. The authors discuss the etiology of dental trauma and the highly psychologic impact of such injuries upon the patient and parents. Techniques for prevention and a comprehensive plan are outlined for systematic history taking and examination. A classification of eight levels of dental injuries (5), techniques for the emergency, and subsequent restorative care are given. Emphasis is placed upon immediate care which can, if necessary, be provided by the physician pending referral to a dentist.
|
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] |
PMID:21304
|
Nonstructural proteins of herpes simplex virus. I. Purification of the induced DNA polymerase.
|
Herpes simplex virus-induced DNA polymerase purified by published methods was found to be contaminated with many others proteins, including virus structural proteins. Thus, DEAE-cellulose and phosphocellulose chromatography were used in combination with affinity chromatography to purify DNA polymerase from herpes simplex virus type 1- and type 2-infected cells. The purified enzyme retained unique features of the herpesvirus-induced DNA polymerase, including a requirement for high salt concentrations for maximal activity, a sensitivity to low phosphonoacetate concentrations, and the capacity to be neutralized by rabbit antiserum to herpesvirus-infected cells. By polyacrylamide gel electrophoresis, the purified DNA polymerase was associated with a virus-induced polypeptide of about 150,000 molecular weight.
|
Nonstructural proteins of herpes simplex virus. I. Purification of the induced DNA polymerase. Herpes simplex virus-induced DNA polymerase purified by published methods was found to be contaminated with many others proteins, including virus structural proteins. Thus, DEAE-cellulose and phosphocellulose chromatography were used in combination with affinity chromatography to purify DNA polymerase from herpes simplex virus type 1- and type 2-infected cells. The purified enzyme retained unique features of the herpesvirus-induced DNA polymerase, including a requirement for high salt concentrations for maximal activity, a sensitivity to low phosphonoacetate concentrations, and the capacity to be neutralized by rabbit antiserum to herpesvirus-infected cells. By polyacrylamide gel electrophoresis, the purified DNA polymerase was associated with a virus-induced polypeptide of about 150,000 molecular weight.
|
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] |
PMID:21305
|
Properties of deoxynucleoside 5'-monophosphatase induced by bacteriophage T5 after infection of Escherichia coli.
|
Bacteriophage T5 induced a deoxynucleoside 5'-monophosphatase during its infection of Escherichia coli. The enzyme was purified about 100-fold. It was clearly distinct from the host 5'-nucleotidase activity in its physical characteristics and substrate specificity. The enzyme was active on deoxynucleoside 5'-monophosphates but was not active as a phosphatase on ribonucleotides, deoxynucleoside 5'-triphosphates, deoxynucleoside 3'-monophosphates, or deoxyoligonucleotides. Furthermore, it did not have oligonucleotidase or exonuclease activity. The enzyme could exist in multimeric form but had a monomer molecular weight of about 25,000.
|
Properties of deoxynucleoside 5'-monophosphatase induced by bacteriophage T5 after infection of Escherichia coli. Bacteriophage T5 induced a deoxynucleoside 5'-monophosphatase during its infection of Escherichia coli. The enzyme was purified about 100-fold. It was clearly distinct from the host 5'-nucleotidase activity in its physical characteristics and substrate specificity. The enzyme was active on deoxynucleoside 5'-monophosphates but was not active as a phosphatase on ribonucleotides, deoxynucleoside 5'-triphosphates, deoxynucleoside 3'-monophosphates, or deoxyoligonucleotides. Furthermore, it did not have oligonucleotidase or exonuclease activity. The enzyme could exist in multimeric form but had a monomer molecular weight of about 25,000.
|
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] |
PMID:21308
|
Renal acidifying ability in subjects with recurrent stone formation.
|
To determine the incidence of an acidification defect in men in whom calcium stones form and its relationship to parathyroid function 120 such patients were given an acute dosage of 0.1 gm. per kg. oral ammonium chloride and circulating immunoreactive parathyroid hormone was determined. The subjects were divided into 2 groups, according to normal or high parathormone levels. Group 1 consisted of 46 men in whom immunoreactive parathyroid hormone was less than or equal to 60 mulEq. per ml. and group 2 consisted of 74 men with immunoreactive parathyroid hormone greater than 60 mulEq. per ml. Of 8 men in whom the urine failed to acidify to less than a pH of 5.3, 3 were from group 1 and 5 were from group 2. None of the patients had an active urinary tract infection. There was no difference in minimal urine pH among the patients in whom the urine acidified normally regardless of immunoreactive parathyroid hormone. The incidence of abnormal acidification in our population was 6% and all of these patients had the incomplete form of renal tubular acidosis. These findings have important therapeutic implications.
|
Renal acidifying ability in subjects with recurrent stone formation. To determine the incidence of an acidification defect in men in whom calcium stones form and its relationship to parathyroid function 120 such patients were given an acute dosage of 0.1 gm. per kg. oral ammonium chloride and circulating immunoreactive parathyroid hormone was determined. The subjects were divided into 2 groups, according to normal or high parathormone levels. Group 1 consisted of 46 men in whom immunoreactive parathyroid hormone was less than or equal to 60 mulEq. per ml. and group 2 consisted of 74 men with immunoreactive parathyroid hormone greater than 60 mulEq. per ml. Of 8 men in whom the urine failed to acidify to less than a pH of 5.3, 3 were from group 1 and 5 were from group 2. None of the patients had an active urinary tract infection. There was no difference in minimal urine pH among the patients in whom the urine acidified normally regardless of immunoreactive parathyroid hormone. The incidence of abnormal acidification in our population was 6% and all of these patients had the incomplete form of renal tubular acidosis. These findings have important therapeutic implications.
|
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] |
PMID:21309
|
The effect of bicarbonate and distilled water on sickle cell trait hematuria and in vitro studies on the interaction of osmolality and pH on erythrocyte sickling in sickle cell trait.
|
The effect of intravenously administered distilled water was examined alone and during alkalization in a patient with gross hematuria associated with the sickle cell trait. On each of 4 occasions hematuria ceased promptly after the infusion of distilled water. Bicarbonate therapy also consistently decreased hematuria. In vitro studies on erythrocytes from another patient with sickle cell trait and hematuria demonstrated that slight increases in urinary pH similar to those that occur in the urine during alkalization can reverse or prevent erythrocyte sickling in the sicle cell trait. If patients with the sickle cell trait are hydrated adequately and have a good rate of urine flow distilled water can be given intravenously with virtually no danger of acute tubular necrosis secondary to erythrocyte hemolysis.
|
The effect of bicarbonate and distilled water on sickle cell trait hematuria and in vitro studies on the interaction of osmolality and pH on erythrocyte sickling in sickle cell trait. The effect of intravenously administered distilled water was examined alone and during alkalization in a patient with gross hematuria associated with the sickle cell trait. On each of 4 occasions hematuria ceased promptly after the infusion of distilled water. Bicarbonate therapy also consistently decreased hematuria. In vitro studies on erythrocytes from another patient with sickle cell trait and hematuria demonstrated that slight increases in urinary pH similar to those that occur in the urine during alkalization can reverse or prevent erythrocyte sickling in the sicle cell trait. If patients with the sickle cell trait are hydrated adequately and have a good rate of urine flow distilled water can be given intravenously with virtually no danger of acute tubular necrosis secondary to erythrocyte hemolysis.
|
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] |
PMID:21310
|
Bilateral seminoma 34 years after orchiopexy.
|
A case of bilateral seminoma in a 59-year-old patient who had undergone bilateral orchiopexy 34 years previously is presented. To our knowledge this is the longest interval between an orchiopexy and diagnosis of bilateral malignancy.
|
Bilateral seminoma 34 years after orchiopexy. A case of bilateral seminoma in a 59-year-old patient who had undergone bilateral orchiopexy 34 years previously is presented. To our knowledge this is the longest interval between an orchiopexy and diagnosis of bilateral malignancy.
|
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] |
PMID:21311
|
Occurrence of rumenitis in a supplementary fed white-tailed deer herd.
|
Rumenitis was observed with increased frequency in a herd of white-tailed deer (Odocoileus virginianus) maintained on a high carbohydrate supplemental ration. Healing rumen scars were found in 4.4% (n=225) of animals examined in 1973; 24.1% (n=278) in 1974; and 42.5% (n=308) in 1975. The lesions often involved nearly the entire ventral blind sac of the rumen. Histopathologic studies did not define the etiologic agent and invasion by either fungi or Fusiformis necrophorus was not a prominent feature in the cases examined. Recovery appeared to be complete and the disease was not considered to be an important herd mortality factor.
|
Occurrence of rumenitis in a supplementary fed white-tailed deer herd. Rumenitis was observed with increased frequency in a herd of white-tailed deer (Odocoileus virginianus) maintained on a high carbohydrate supplemental ration. Healing rumen scars were found in 4.4% (n=225) of animals examined in 1973; 24.1% (n=278) in 1974; and 42.5% (n=308) in 1975. The lesions often involved nearly the entire ventral blind sac of the rumen. Histopathologic studies did not define the etiologic agent and invasion by either fungi or Fusiformis necrophorus was not a prominent feature in the cases examined. Recovery appeared to be complete and the disease was not considered to be an important herd mortality factor.
|
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-0.08889146149158478,
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] |
PMID:21318
|
Demonstration of vaccinia virus antigen in brains of postvaccinal encephalitis cases.
|
Five lethal cases of postovaccinal encephalitis (PVE) were examined in attempts to detect the viral antigen by the fluorescent antibody techniques and to isolate the infectious vaccinia virus. Histologically, the brain tissues were characterized by meningoencephalitis, with perivascular infiltrations and inflammatous reactions mainly in leptomininx, chroid plexus and ependyma. By direct immunofluorescence staining, vaccinia virus antigen was found in the brain specimens of one case, but not in the other four cases. The existence of antigen-antibody complexes was suggested by the deposition of immunoglobulins in the brain specimens. After treatment with 3 M NaSCN solution to dissociate the immunoglobulins from the complex, the viral antigen was demonstrated in specimens of two cases. Localization of viral antigen(s) thus detected coincided with that of meningoencephalitic reactions in the histological examination. Virus isolation on chick embryo chorioallantoic membrane was negative in all cases. Participation of viral pathogenicity in the etiology of PVE is discussed.
|
Demonstration of vaccinia virus antigen in brains of postvaccinal encephalitis cases. Five lethal cases of postovaccinal encephalitis (PVE) were examined in attempts to detect the viral antigen by the fluorescent antibody techniques and to isolate the infectious vaccinia virus. Histologically, the brain tissues were characterized by meningoencephalitis, with perivascular infiltrations and inflammatous reactions mainly in leptomininx, chroid plexus and ependyma. By direct immunofluorescence staining, vaccinia virus antigen was found in the brain specimens of one case, but not in the other four cases. The existence of antigen-antibody complexes was suggested by the deposition of immunoglobulins in the brain specimens. After treatment with 3 M NaSCN solution to dissociate the immunoglobulins from the complex, the viral antigen was demonstrated in specimens of two cases. Localization of viral antigen(s) thus detected coincided with that of meningoencephalitic reactions in the histological examination. Virus isolation on chick embryo chorioallantoic membrane was negative in all cases. Participation of viral pathogenicity in the etiology of PVE is discussed.
|
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0.01751568354666233,
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] |
PMID:21319
|
Prostaglandin synthetase systems in rat and rabbit renal medulla and inhibition by non-steroidal anti-inflammatory drugs.
|
The properties of prostaglandin synthetase systems (PSSs) in the renal medulla of the rat and rabbit, and inhibition by ketoprofen, indomethacin, ibuprofen, phenylbutazone and aspirin were investigated in relation to their anti-inflammatory, analgesic, antipyretic and ulcerogenic activities. Rat and rabbit PSSs produced prostaglandin (PG)E and PGF from arachidonic and dihomo-gamma-linolenic acids and had an optimal pH of 8.5 and 7.5 for PGE formation, respectively. Only a slight loss of activity occurred with lyophilization. In the rat PSS, all drugs tested were inhibitory in the order of ketoprofen, ibuprofen, indomethacin and aspirin, respectively. In the rabbit PSS, the same potency relationship was also found. Drug sensitivity of the rat PSS was remarkably lower than that of the rabbit PSS. Significant correlations were noted between the inhibitory potencies of the drugs against both PSSs and other in vivo pharmacological activities within the same species.
|
Prostaglandin synthetase systems in rat and rabbit renal medulla and inhibition by non-steroidal anti-inflammatory drugs. The properties of prostaglandin synthetase systems (PSSs) in the renal medulla of the rat and rabbit, and inhibition by ketoprofen, indomethacin, ibuprofen, phenylbutazone and aspirin were investigated in relation to their anti-inflammatory, analgesic, antipyretic and ulcerogenic activities. Rat and rabbit PSSs produced prostaglandin (PG)E and PGF from arachidonic and dihomo-gamma-linolenic acids and had an optimal pH of 8.5 and 7.5 for PGE formation, respectively. Only a slight loss of activity occurred with lyophilization. In the rat PSS, all drugs tested were inhibitory in the order of ketoprofen, ibuprofen, indomethacin and aspirin, respectively. In the rabbit PSS, the same potency relationship was also found. Drug sensitivity of the rat PSS was remarkably lower than that of the rabbit PSS. Significant correlations were noted between the inhibitory potencies of the drugs against both PSSs and other in vivo pharmacological activities within the same species.
|
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] |
PMID:21321
|
[Evaluation of antireflux effect of fundic patch operation by withdrawal pH curve (author's transl)].
|
With the use of gastroesophageal withdrawal pH curve, pathophysiology after various surgical procedures for achalasia of the esophagus was investigated experimentally from the view point of postoperative reflux. A total of 68 dogs were divided into four groups and were prepared with proximal gastrectomy with end-to-end esophagogastrostomy, Wendel procedure, Heller procedure and Fundic patch operation, respectively. In the group with Fundic patch operation, efficacy of the flap valve, mucosal valve and fundoplication was also evaluated preparing them in various sizes. The results obtained may be summarized as follows: 1) Withdrawal pH measurement is a sentive mean to detect the gastroesophageal reflux. 2) Proximal gastrectomy with end-to-end esophagogastrostomy and Wendel procedure yielded worst results with severe gastroesophageal reflux. On the contrary, Fundic patch operation best controlled the gastroesophageal reflux. 3) Gastroesophageal reflux could be prevented by the Fundic patch operation with the flap valve 6 cm in length and fundoplication enclosing around 1/2 to 2/3 circumference of the distal esophagus.
|
[Evaluation of antireflux effect of fundic patch operation by withdrawal pH curve (author's transl)]. With the use of gastroesophageal withdrawal pH curve, pathophysiology after various surgical procedures for achalasia of the esophagus was investigated experimentally from the view point of postoperative reflux. A total of 68 dogs were divided into four groups and were prepared with proximal gastrectomy with end-to-end esophagogastrostomy, Wendel procedure, Heller procedure and Fundic patch operation, respectively. In the group with Fundic patch operation, efficacy of the flap valve, mucosal valve and fundoplication was also evaluated preparing them in various sizes. The results obtained may be summarized as follows: 1) Withdrawal pH measurement is a sentive mean to detect the gastroesophageal reflux. 2) Proximal gastrectomy with end-to-end esophagogastrostomy and Wendel procedure yielded worst results with severe gastroesophageal reflux. On the contrary, Fundic patch operation best controlled the gastroesophageal reflux. 3) Gastroesophageal reflux could be prevented by the Fundic patch operation with the flap valve 6 cm in length and fundoplication enclosing around 1/2 to 2/3 circumference of the distal esophagus.
|
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] |
PMID:21323
|
[Prostaglandin E1: effect on blood gases in infants with cyanotic congenital heart disease (author's transl)].
|
15 infants with cyanotic congenital heart disease (pulmonary atresia, Ebstein-Syndrom) were treated with Prostaglandin E1. During treatment there was a significant rise of PO2 and SO2 in the arterial, capillary and central venous blood. There was a minor rise of pH and HCO3; the arterial pCO2 fell slightly. We used PGE1-therapy as pretreatment before the heart operation, so that the critical babies go to the operation well oxygenated and in a better state. The side effects we observed (tachypnoe, tachycardia, hyperpyrexia, augmented urine output, erythemas, apnoic spells) seemed less important than the great advantage of a better oxygenation of these hypoxic babies.
|
[Prostaglandin E1: effect on blood gases in infants with cyanotic congenital heart disease (author's transl)]. 15 infants with cyanotic congenital heart disease (pulmonary atresia, Ebstein-Syndrom) were treated with Prostaglandin E1. During treatment there was a significant rise of PO2 and SO2 in the arterial, capillary and central venous blood. There was a minor rise of pH and HCO3; the arterial pCO2 fell slightly. We used PGE1-therapy as pretreatment before the heart operation, so that the critical babies go to the operation well oxygenated and in a better state. The side effects we observed (tachypnoe, tachycardia, hyperpyrexia, augmented urine output, erythemas, apnoic spells) seemed less important than the great advantage of a better oxygenation of these hypoxic babies.
|
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] |
PMID:21324
|
Detection of circulating immune complexes with a modified Raji cell technique.
|
A modification of the Raji cell technique for the detection of circulating immune complexes is described. Raji lymphoid cells bind immune complexes via the C 3 receptor. Prior to incubation with the test serum it is necessary to block the IgG Fc receptor which would interfere with the assay. In the present modification the IgG Fc receptor is blocked with monoclonal IgG myeloma proteins thereby facilitating the detection of C 3 bound immune complexes with fluoresecein-conjugated anti-light chain serum. This modification is presently used in a survey of immune complexes in a number of autoimmune diseases.
|
Detection of circulating immune complexes with a modified Raji cell technique. A modification of the Raji cell technique for the detection of circulating immune complexes is described. Raji lymphoid cells bind immune complexes via the C 3 receptor. Prior to incubation with the test serum it is necessary to block the IgG Fc receptor which would interfere with the assay. In the present modification the IgG Fc receptor is blocked with monoclonal IgG myeloma proteins thereby facilitating the detection of C 3 bound immune complexes with fluoresecein-conjugated anti-light chain serum. This modification is presently used in a survey of immune complexes in a number of autoimmune diseases.
|
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] |
PMID:21325
|
Polyanion and complement receptor of the glomerular epithelium. Relationship to pH.
|
Two markers on the surface of glomerular epithelial cells were studied on human and rat tissue. The glomerular polyanion is known to be a sialoglycoprotein present profusely on glomerular epithelial cell surfaces, and it is detected by binding with cationic dyes. This staining is lost after incubation in the pH range 3.8 to 4.4, yet retained at a more acidic or physiologic pH. A receptor for complement is also present on human glomerular epithelial cells. This receptor is also lost as a function of varying pH incubation and this loss parallels the pattern observed for glomerular polyanion. Neuraminidase treatment of renal tissue removes the sialic acid-dependent glomerular polyanion staining but preserves and stabilizes the complement receptor. Both functions are markers of the cell surface of glomerular epithelial cells and behave as peripheral membrane proteins.
|
Polyanion and complement receptor of the glomerular epithelium. Relationship to pH. Two markers on the surface of glomerular epithelial cells were studied on human and rat tissue. The glomerular polyanion is known to be a sialoglycoprotein present profusely on glomerular epithelial cell surfaces, and it is detected by binding with cationic dyes. This staining is lost after incubation in the pH range 3.8 to 4.4, yet retained at a more acidic or physiologic pH. A receptor for complement is also present on human glomerular epithelial cells. This receptor is also lost as a function of varying pH incubation and this loss parallels the pattern observed for glomerular polyanion. Neuraminidase treatment of renal tissue removes the sialic acid-dependent glomerular polyanion staining but preserves and stabilizes the complement receptor. Both functions are markers of the cell surface of glomerular epithelial cells and behave as peripheral membrane proteins.
|
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] |
PMID:21329
|
On the inactivation of hepatic tyrosine aminotransferase.
|
Tyrosine aminotransferase from frog liver requires no exogenous pyridoxal-5'-phosphate for maximum activity. The cofactor cannot be removed from the enzyme by dialysis as in the case of the rat enzyme. Pyridoxal phosphate also fails to elevate frog liver tyrosine aminotransferase activity in vivo. The enzyme activity decreases rapidly after administration of cycloheximide, which indicates that its turnover is rapid. These results strongly contradict the cofactor-dependent model of enzyme degradation. Rat and frog liver tyrosine aminotransferases are stable in neutral homogenates at 37 degrees C but are rapidly inactivated after addition of cysteine in millimolar concentrations. This effect is probably due to cystine formed during the incubation. The rates of inactivation of the different subforms of the enzyme in this system were identical. No membrane-bound system is needed for the inactivation by cystine. It is possible that the denaturation occurs by sulfide exchange. Fructose and glucose lower the enzyme activity in both rat and frog liver to an equal extent. This effect is not due to instability of the enzyme activity in both rat and frog liver to an equal extent. This effect is not due to instability of the enzyme in the presence of sugars of their metabolites. Theories on the inactivation of enzymes will be discussed in the light of the present results.
|
On the inactivation of hepatic tyrosine aminotransferase. Tyrosine aminotransferase from frog liver requires no exogenous pyridoxal-5'-phosphate for maximum activity. The cofactor cannot be removed from the enzyme by dialysis as in the case of the rat enzyme. Pyridoxal phosphate also fails to elevate frog liver tyrosine aminotransferase activity in vivo. The enzyme activity decreases rapidly after administration of cycloheximide, which indicates that its turnover is rapid. These results strongly contradict the cofactor-dependent model of enzyme degradation. Rat and frog liver tyrosine aminotransferases are stable in neutral homogenates at 37 degrees C but are rapidly inactivated after addition of cysteine in millimolar concentrations. This effect is probably due to cystine formed during the incubation. The rates of inactivation of the different subforms of the enzyme in this system were identical. No membrane-bound system is needed for the inactivation by cystine. It is possible that the denaturation occurs by sulfide exchange. Fructose and glucose lower the enzyme activity in both rat and frog liver to an equal extent. This effect is not due to instability of the enzyme activity in both rat and frog liver to an equal extent. This effect is not due to instability of the enzyme in the presence of sugars of their metabolites. Theories on the inactivation of enzymes will be discussed in the light of the present results.
|
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] |
PMID:21328
|
Model membranes for the study of active transport phenomena.
|
Models for active transport are prepared by the covalent bonding of molecules containing a catalytic site to the membrane asymmetrically with respect to its thickness. The membrane separates two compartments of unequal volume, both initially containing reactant at the same concentration. We observed the time dependence of the reactant and product concentrations, and of the osmotic pressure, and these results are compared with theoretical predictions. The two reactions studied are the hydrolysis of ethyl N-acetyl-L-tyrosinate catalyzed by alpha-chymotrypsin and the acid-catalyzed hydrolysis of triethoxymethane. The asymmetric membrane consumes reactant, and discharges product, at different rates through its two faces. The concentration of products, and of non-rate determining reactants, may exhibit maxima or minima with time, and computer simulation indicates that oscillatory behavior could be expected under appropriate conditions. Due to the different exit path lengths, the osmotic response (determined by the solute concentrations at the two membrane surfaces) may be opposite in sign to that expected from the concentrations in the external compartments.
|
Model membranes for the study of active transport phenomena. Models for active transport are prepared by the covalent bonding of molecules containing a catalytic site to the membrane asymmetrically with respect to its thickness. The membrane separates two compartments of unequal volume, both initially containing reactant at the same concentration. We observed the time dependence of the reactant and product concentrations, and of the osmotic pressure, and these results are compared with theoretical predictions. The two reactions studied are the hydrolysis of ethyl N-acetyl-L-tyrosinate catalyzed by alpha-chymotrypsin and the acid-catalyzed hydrolysis of triethoxymethane. The asymmetric membrane consumes reactant, and discharges product, at different rates through its two faces. The concentration of products, and of non-rate determining reactants, may exhibit maxima or minima with time, and computer simulation indicates that oscillatory behavior could be expected under appropriate conditions. Due to the different exit path lengths, the osmotic response (determined by the solute concentrations at the two membrane surfaces) may be opposite in sign to that expected from the concentrations in the external compartments.
|
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] |
PMID:21340
|
Use of prazosin at the dunedin hypertension clinic controlled and open studies and pharmacokinetic observations.
|
Prazosin has been used as an antihypertensive drug in the treatment of 93 patients in Dunedin since 1971-1972, mainly those whose previous control was unsatisfactory. It has led to very significant improvement of control in many cases; 48 patients now receiving the drug have taken it for an average of 30 months. Forty-five patients have stopped taking the drug for various reasons, such as failure to respond (11-8%), side effects (20-4%), myocardial infarction (8-6%) or unrelated reasons (7-5%). This reflects to some extent the use ofa new drug in patients who are difficult to control, and its use initially without concomitant diuretic and beta-blocker therapy. We believe that the place of praxosin is primarily as a third drug for patients whose hypertension does not respond satisfactorirly to a diuretic and a beta-blocker. The first dose must be kept small, preferably 0-25 mg, and even with this dose a small proportion of patients receiving diuretic and beta-blocker therapy seem to become hypotensive; patients should be warned about this. The plasma half-life in normal volunteers was 3-8 hours but in some patients it seems to be considerably longer.
|
Use of prazosin at the dunedin hypertension clinic controlled and open studies and pharmacokinetic observations. Prazosin has been used as an antihypertensive drug in the treatment of 93 patients in Dunedin since 1971-1972, mainly those whose previous control was unsatisfactory. It has led to very significant improvement of control in many cases; 48 patients now receiving the drug have taken it for an average of 30 months. Forty-five patients have stopped taking the drug for various reasons, such as failure to respond (11-8%), side effects (20-4%), myocardial infarction (8-6%) or unrelated reasons (7-5%). This reflects to some extent the use ofa new drug in patients who are difficult to control, and its use initially without concomitant diuretic and beta-blocker therapy. We believe that the place of praxosin is primarily as a third drug for patients whose hypertension does not respond satisfactorirly to a diuretic and a beta-blocker. The first dose must be kept small, preferably 0-25 mg, and even with this dose a small proportion of patients receiving diuretic and beta-blocker therapy seem to become hypotensive; patients should be warned about this. The plasma half-life in normal volunteers was 3-8 hours but in some patients it seems to be considerably longer.
|
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0.06996303796768188,
-0.04775695875287056,
-0.025263814255595207,
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0.047132860869169235,
0.044260572642087936,
0.045333221554756165
] |
PMID:21345
|
[On the action of antihypotensive agents in sympathicotonic orthostatic hypotension in geriartric patients: comparison between placebo and etilefrin (author's transl)].
|
The action of etilefrin (Effortil Depot Perlongets) was compared with placebo in a double-blind study in 24 female geriatric patients with sympathicotonic orthostatic hypotension. After determining the basic values, all patients were treated with the active substance in a titration phase lasting one week (dosage 2-3 Perlongets/day). The decrease in systolic blood pressure and the increase in pulse rate while standing were then statistically significant lower (p less than (p less than 0.001) when compared with the basic values. In 17 out of 21 cases of collapse which occured while standing before therapy was commenced no further collapse occurred (p less than 0.005). Following the titration phase treatment with etilefrin was continued in 12 patients in a double-blind study while the remaining 12 patients were changed over to placebo as a withdrawal study. The effect continued in those patients treated with the active ingredient and the average values and incidence of effects improved further. On the other hand, in the placebo group there was one again a marked decrease in systolic blood pressure and increase in pulse rate as observed in the basic values. The symptomatology, particulary episodes of collapse increased again. There was a statistically significant difference between the action of etilefrin and placebo for all criteria (both objective and subjective parameters). Side-effects were not observed.
|
[On the action of antihypotensive agents in sympathicotonic orthostatic hypotension in geriartric patients: comparison between placebo and etilefrin (author's transl)]. The action of etilefrin (Effortil Depot Perlongets) was compared with placebo in a double-blind study in 24 female geriatric patients with sympathicotonic orthostatic hypotension. After determining the basic values, all patients were treated with the active substance in a titration phase lasting one week (dosage 2-3 Perlongets/day). The decrease in systolic blood pressure and the increase in pulse rate while standing were then statistically significant lower (p less than (p less than 0.001) when compared with the basic values. In 17 out of 21 cases of collapse which occured while standing before therapy was commenced no further collapse occurred (p less than 0.005). Following the titration phase treatment with etilefrin was continued in 12 patients in a double-blind study while the remaining 12 patients were changed over to placebo as a withdrawal study. The effect continued in those patients treated with the active ingredient and the average values and incidence of effects improved further. On the other hand, in the placebo group there was one again a marked decrease in systolic blood pressure and increase in pulse rate as observed in the basic values. The symptomatology, particulary episodes of collapse increased again. There was a statistically significant difference between the action of etilefrin and placebo for all criteria (both objective and subjective parameters). Side-effects were not observed.
|
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] |
PMID:21348
|
Mutagenesis by simian virus 40. II. Changes in substrate affinities in mutant hypoxanthine-guanine phosphoribosyl transferase enzymes at different pH values.
|
A number of 8-azaguanine-resistant clones selected from Chinese hamster cells infected with SV 40, and supposed to originate by virus infection was investigated to demonstrate and analyze genetic alterations occurring in the cells after infection. All resistant clones tested showed reduced but detectable activity levels of the enzyme hypoxanthine-guanine phosphoribosyltransferase. The extent of reduction in the activity was not identical for different substrates. In all the clones tested, spontaneous mutants included, the pH optimum for the enzymic reaction with guanine was shifted to lower values. The reduced enzymic activities of resistant clones correlated with their colony-forming ability in corresponding selective media. The results support the suggestion that SV 40 is able to induce gene mutations.
|
Mutagenesis by simian virus 40. II. Changes in substrate affinities in mutant hypoxanthine-guanine phosphoribosyl transferase enzymes at different pH values. A number of 8-azaguanine-resistant clones selected from Chinese hamster cells infected with SV 40, and supposed to originate by virus infection was investigated to demonstrate and analyze genetic alterations occurring in the cells after infection. All resistant clones tested showed reduced but detectable activity levels of the enzyme hypoxanthine-guanine phosphoribosyltransferase. The extent of reduction in the activity was not identical for different substrates. In all the clones tested, spontaneous mutants included, the pH optimum for the enzymic reaction with guanine was shifted to lower values. The reduced enzymic activities of resistant clones correlated with their colony-forming ability in corresponding selective media. The results support the suggestion that SV 40 is able to induce gene mutations.
|
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] |
PMID:21349
|
Bacterial stimulation and granulocyte inhibition of granulopoietic factor production.
|
We attempted to determine the effect of live bacteria (Staphylococcus epidermidis) on granulocyte colony-stimulating-factor production by human peripheral blood mononuclear cells (monocytes and lymphocytes) in vitro. Addition of bacteria to mononuclear-cell cultures enhanced colony-stimulating-factor production by these cells, as assayed on both human and mouse bone marrow. Addition of peripheral blood granulocytes to parallel cultures eliminated this enhancement effect, presumably by bacterial removal or inactivation. These data suggest that micro-organisms may have a pivotal role in granulocyte production and maturation by serving as a stimulus to increase colony-stimulating-factor production and also as negative control through their removal by the newly formed granulocytes.
|
Bacterial stimulation and granulocyte inhibition of granulopoietic factor production. We attempted to determine the effect of live bacteria (Staphylococcus epidermidis) on granulocyte colony-stimulating-factor production by human peripheral blood mononuclear cells (monocytes and lymphocytes) in vitro. Addition of bacteria to mononuclear-cell cultures enhanced colony-stimulating-factor production by these cells, as assayed on both human and mouse bone marrow. Addition of peripheral blood granulocytes to parallel cultures eliminated this enhancement effect, presumably by bacterial removal or inactivation. These data suggest that micro-organisms may have a pivotal role in granulocyte production and maturation by serving as a stimulus to increase colony-stimulating-factor production and also as negative control through their removal by the newly formed granulocytes.
|
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] |
PMID:21351
|
Reconstitution in severe combined immunodeficiency by transplantation of marrow from an unrelated donor.
|
A patient with severe combined immunodeficiency received seven transplants of bone marrow from an HLA-B-compatible and HLA-D-compatible unrelated donor in an attempt to provide immunologic reconstitution. The first four transplants achieved restricted engraftment with evidence of rudimentary immunologic function. A fifth transplant, given after low-dose cyclophosphamide, produced reconstituion of cell-mediated immunity. Marrow aplasia developed after recontamination with a nonpathogenic microflora. Transplantation of marrow previously stored in liquid nitrogen was ineffective. A subsequent transplant, administered after high-dose cyclophosphamide, achieved durable engraftment, with complete hematopoietic and immunologic reconstitution. Seventeen months after transplantation, full functional engraftment persists. Graft-versus-host disease has been chronic and moderately severe, but limited to the skin and oral mucosa. Transplantation of marrow from unrelated histocompatible donors may provide a useful treatment for patients with severe combined immunodeficiency or aplastic anemia who lack a matched sibling or related donor.
|
Reconstitution in severe combined immunodeficiency by transplantation of marrow from an unrelated donor. A patient with severe combined immunodeficiency received seven transplants of bone marrow from an HLA-B-compatible and HLA-D-compatible unrelated donor in an attempt to provide immunologic reconstitution. The first four transplants achieved restricted engraftment with evidence of rudimentary immunologic function. A fifth transplant, given after low-dose cyclophosphamide, produced reconstituion of cell-mediated immunity. Marrow aplasia developed after recontamination with a nonpathogenic microflora. Transplantation of marrow previously stored in liquid nitrogen was ineffective. A subsequent transplant, administered after high-dose cyclophosphamide, achieved durable engraftment, with complete hematopoietic and immunologic reconstitution. Seventeen months after transplantation, full functional engraftment persists. Graft-versus-host disease has been chronic and moderately severe, but limited to the skin and oral mucosa. Transplantation of marrow from unrelated histocompatible donors may provide a useful treatment for patients with severe combined immunodeficiency or aplastic anemia who lack a matched sibling or related donor.
|
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] |
PMID:21354
|
[Information transmission by means of neurosecretory peptides as mediators].
|
Morphological indications and new experimental results demonstrate that neurosecretory peptides or low-molecular proteins, respectively, appear to effect as mediators in information transmission. They are acting as releasers triggering specific behavior programs in the nervous system or as modulators in the regulation of different functions. This can be observed in different groups of the animal kingdom including mammals and man as well as different levels of organization or systems. Some of such facts at behavior level, concerning regulation of organ function and finally at cellular level of distinct single neurons are discussed.
|
[Information transmission by means of neurosecretory peptides as mediators]. Morphological indications and new experimental results demonstrate that neurosecretory peptides or low-molecular proteins, respectively, appear to effect as mediators in information transmission. They are acting as releasers triggering specific behavior programs in the nervous system or as modulators in the regulation of different functions. This can be observed in different groups of the animal kingdom including mammals and man as well as different levels of organization or systems. Some of such facts at behavior level, concerning regulation of organ function and finally at cellular level of distinct single neurons are discussed.
|
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] |
PMID:21371
|
[Possibilities of treatment of maldescensus testis in the dog (author's transl)].
|
The diagnosis of inguinal retention of the testis can be made in the dog from the 10th week of life. Like in man, therapy of this condition can be done with gonadotropins or releasing hormones. In conditions with retention of the testicles in the upper inguinal region LH-RH proved to be more successful than gonadotropin. 10 out of 16 patients showed a complete descent of the testes. In addition the effect of plasmagonadotropin as well as urinary chorionic gonadotropin, and of LH-RH on the plasma testosterone levels of juvenile and adult dogs was studied. It could be seen that in the young dogs all 3 hormones caused an increase in plasma testosterone, while in the adult animal only LH-RH was able to produce a significant rise.
|
[Possibilities of treatment of maldescensus testis in the dog (author's transl)]. The diagnosis of inguinal retention of the testis can be made in the dog from the 10th week of life. Like in man, therapy of this condition can be done with gonadotropins or releasing hormones. In conditions with retention of the testicles in the upper inguinal region LH-RH proved to be more successful than gonadotropin. 10 out of 16 patients showed a complete descent of the testes. In addition the effect of plasmagonadotropin as well as urinary chorionic gonadotropin, and of LH-RH on the plasma testosterone levels of juvenile and adult dogs was studied. It could be seen that in the young dogs all 3 hormones caused an increase in plasma testosterone, while in the adult animal only LH-RH was able to produce a significant rise.
|
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] |
PMID:21372
|
Comparative study of beta andreoceptor antagonists on the isolated atria of control and of the reserpine treated rabbits.
|
The effect of four adrenoceptor antagonists, chosen because of reported differences in their selectivities, were compared using the positive chronotropic response to isoprenaline on isolated rabbit atria. Oxprenolol was the most potent antagonist of the isoprenaline induced cardiac arrhythmias. Alprenolol, practolol and propranolol also blocked the positive chronotropic responses to isoprenaline effectively. All the antagonists lowered the resting heart rate. The effects of all four selected antagonists on heart rate probably result from cardiac beta adrenoceptor blockade. Atria isolated from reserpine treated rabbits, showed a reduced percentage of increase in the heart rate in response to addition of isoprenaline. This decreased response has been related in some cases to direct myocardial inhibition.
|
Comparative study of beta andreoceptor antagonists on the isolated atria of control and of the reserpine treated rabbits. The effect of four adrenoceptor antagonists, chosen because of reported differences in their selectivities, were compared using the positive chronotropic response to isoprenaline on isolated rabbit atria. Oxprenolol was the most potent antagonist of the isoprenaline induced cardiac arrhythmias. Alprenolol, practolol and propranolol also blocked the positive chronotropic responses to isoprenaline effectively. All the antagonists lowered the resting heart rate. The effects of all four selected antagonists on heart rate probably result from cardiac beta adrenoceptor blockade. Atria isolated from reserpine treated rabbits, showed a reduced percentage of increase in the heart rate in response to addition of isoprenaline. This decreased response has been related in some cases to direct myocardial inhibition.
|
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] |
PMID:21378
|
Arginine esterase and lysosomal hydrolases in liver from cystic fibrosis subjects.
|
The total activity and isoelectric focusing patterns of arginine esterase, cathepsin B1, and several lysosomal hydrolases were normal in liver from two patients with cystic fibrosis. No abnormalities were observed in values for pH optimum, Km, and Vmax for arginine esterase and cathepsin B1 in liver from cystic fibrosis patients compared to those values for liver from the control subject. Soybean trypsin inhibitor at concentrations up to 100 microgram/ml had no effect on liver arginine esterase or cathepsin B1.
|
Arginine esterase and lysosomal hydrolases in liver from cystic fibrosis subjects. The total activity and isoelectric focusing patterns of arginine esterase, cathepsin B1, and several lysosomal hydrolases were normal in liver from two patients with cystic fibrosis. No abnormalities were observed in values for pH optimum, Km, and Vmax for arginine esterase and cathepsin B1 in liver from cystic fibrosis patients compared to those values for liver from the control subject. Soybean trypsin inhibitor at concentrations up to 100 microgram/ml had no effect on liver arginine esterase or cathepsin B1.
|
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] |
PMID:21381
|
Problems in assessment of vividness and control of imagery.
|
Difficulties in assessing individual differences in vividness and control of mental imagery hinder understanding of the role of of imagery in various phenomena. This study examined the relationships among the Gordon test of imagery control, the Betts questionnaire on imagery vividness, and a research questionnaire on control of imagery developed for this study. The research questionnaire demonstrated satisfactory internal consistency and scores were more widely distributed than were those on the Gordon test. Correlations among the instruments ranged from .47 to .57, suggesting that vividness and control of imagery are not clearly differentiated in practice. Discussion of these results suggests that further empirical work is needed to establish the differential validity of the two constructs.
|
Problems in assessment of vividness and control of imagery. Difficulties in assessing individual differences in vividness and control of mental imagery hinder understanding of the role of of imagery in various phenomena. This study examined the relationships among the Gordon test of imagery control, the Betts questionnaire on imagery vividness, and a research questionnaire on control of imagery developed for this study. The research questionnaire demonstrated satisfactory internal consistency and scores were more widely distributed than were those on the Gordon test. Correlations among the instruments ranged from .47 to .57, suggesting that vividness and control of imagery are not clearly differentiated in practice. Discussion of these results suggests that further empirical work is needed to establish the differential validity of the two constructs.
|
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] |
PMID:21382
|
Heat stable inhibitors produced in raw milk.
|
Twenty raw farm milk samples were tested for inhibitory substances before and after being kept at room temperature until the pH fell to less than 6.3 but greater than 6.2. The tests were done using the IDF-method and the commercial Thermocult method. In both methods B. stearothermophilus var. chalidolactis is used as the test organism. In two instances a thermostable inhibitor was produced with an inhibitory potential greater than 0.01 IU/ml penicillin standard. The IDF-method was found unsuitable for the study of relatively small concentrations of antibiotics or other chemotherapeutics in milk.
|
Heat stable inhibitors produced in raw milk. Twenty raw farm milk samples were tested for inhibitory substances before and after being kept at room temperature until the pH fell to less than 6.3 but greater than 6.2. The tests were done using the IDF-method and the commercial Thermocult method. In both methods B. stearothermophilus var. chalidolactis is used as the test organism. In two instances a thermostable inhibitor was produced with an inhibitory potential greater than 0.01 IU/ml penicillin standard. The IDF-method was found unsuitable for the study of relatively small concentrations of antibiotics or other chemotherapeutics in milk.
|
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] |
PMID:21383
|
[Septicemia in the elderly (author's transl)].
|
Out of 1,251 patients above 65 years of age staying at the Charles Foix Hospital (prolonged hospitalization) and the St. Joseph Hospital (acute cases), 168 had one or more positive blood cultures. Urinary tract infection is a major source of septicemia due to gram negative bacilli. It is important to stress cases of septicemia due to pneumococcal pneumoniae, eschars, and other skin lesions. Mortality varies between 33 and 36%, depending upon the hospital. Collapse, although infrequent, still portends a grave prognosis (61% of cases of collapse led to death at Charles Foix Hospital). The combination of more than two risk factors considerably worsens the prognosis. Hypoproteinemia and dementia are every bit as grave as diabetes and cancer. A better isolation of the microorganisms involved in cases of septicemia in the elderly will lead to a more judicious choice of antibiotics. The administration of chemotherapy immediately after the samples were obtained remains the main guarantee of successful therapy.
|
[Septicemia in the elderly (author's transl)]. Out of 1,251 patients above 65 years of age staying at the Charles Foix Hospital (prolonged hospitalization) and the St. Joseph Hospital (acute cases), 168 had one or more positive blood cultures. Urinary tract infection is a major source of septicemia due to gram negative bacilli. It is important to stress cases of septicemia due to pneumococcal pneumoniae, eschars, and other skin lesions. Mortality varies between 33 and 36%, depending upon the hospital. Collapse, although infrequent, still portends a grave prognosis (61% of cases of collapse led to death at Charles Foix Hospital). The combination of more than two risk factors considerably worsens the prognosis. Hypoproteinemia and dementia are every bit as grave as diabetes and cancer. A better isolation of the microorganisms involved in cases of septicemia in the elderly will lead to a more judicious choice of antibiotics. The administration of chemotherapy immediately after the samples were obtained remains the main guarantee of successful therapy.
|
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] |
PMID:21384
|
[Hereditary deficiency in the enzymes of the biosynthesis of collagen. The Ehlers-Danlos syndromes (author's transl)].
|
The mechanism of the biosynthetic pathway of collagen is briefly summarised. The hereditary enzyme deficiencies of this pathway concern some of the Ehlers-Danlos syndromes. Seven clinically well defined varieties of these syndromes have been recognized, all presenting, as common feature, an hyperextensivitry of joints and hyperelastic, excessively fragile skin. In three of these seven varieties, the enzyme defect has been recently discovered: the type V (associated with chromosome X) is characterized by the deficiency in the lysyl-oxidase, the type VI (ocular) by the deficiency in lysyl-hydroylase; in the type VII (arthrolaxis multiplex congenita) the activity of tropocollagen-peptidase is practically absent. These enzyme deficiencies provide a molecular basis for the interpretation of the pathogenesis of these varieties of the Ehlers-Danlos syndrome.
|
[Hereditary deficiency in the enzymes of the biosynthesis of collagen. The Ehlers-Danlos syndromes (author's transl)]. The mechanism of the biosynthetic pathway of collagen is briefly summarised. The hereditary enzyme deficiencies of this pathway concern some of the Ehlers-Danlos syndromes. Seven clinically well defined varieties of these syndromes have been recognized, all presenting, as common feature, an hyperextensivitry of joints and hyperelastic, excessively fragile skin. In three of these seven varieties, the enzyme defect has been recently discovered: the type V (associated with chromosome X) is characterized by the deficiency in the lysyl-oxidase, the type VI (ocular) by the deficiency in lysyl-hydroylase; in the type VII (arthrolaxis multiplex congenita) the activity of tropocollagen-peptidase is practically absent. These enzyme deficiencies provide a molecular basis for the interpretation of the pathogenesis of these varieties of the Ehlers-Danlos syndrome.
|
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] |
PMID:21388
|
Outpatient management of pediatric surgical problems.
|
A number of pediatric surgical problems commonly seen in the outpatient department or physician's office are reviewed. It is particularly important for the primary care physician to recognize the difficulty of accurate diagnosis in children and the advantage of sedation in improving patient cooperation. Hospitalization may be necessary for adequate observation, proper preparation for diagnostic studies, or safe treatment. Simple traumatic injuries or infections can usually be treated effectively without hospitalization if sound surgical principles are observed. Abdominal pain or rectal bleeding calls for a careful investigation for early signs of inflammatory disease or life-threatening lesions requiring surgical treatment.
|
Outpatient management of pediatric surgical problems. A number of pediatric surgical problems commonly seen in the outpatient department or physician's office are reviewed. It is particularly important for the primary care physician to recognize the difficulty of accurate diagnosis in children and the advantage of sedation in improving patient cooperation. Hospitalization may be necessary for adequate observation, proper preparation for diagnostic studies, or safe treatment. Simple traumatic injuries or infections can usually be treated effectively without hospitalization if sound surgical principles are observed. Abdominal pain or rectal bleeding calls for a careful investigation for early signs of inflammatory disease or life-threatening lesions requiring surgical treatment.
|
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] |
PMID:21390
|
[Influence of pH on nisin production by Streptococcus lactis cultures].
|
The pH effect on the nisine biosynthesis during the cultivation of Streptococcus lactis was studied at pH 5,8 6,7 and 7,2. The pH maintenance at the specified level did not stimulate the growth of Str. lactis, did not increase the total yield of nisine and did not produce a significant effect on the level or cellular nisine. This indicates an important physiological difference between the culture-nisine producer described by Hirsh and our culture Str. lactis, str. Moscow University.
|
[Influence of pH on nisin production by Streptococcus lactis cultures]. The pH effect on the nisine biosynthesis during the cultivation of Streptococcus lactis was studied at pH 5,8 6,7 and 7,2. The pH maintenance at the specified level did not stimulate the growth of Str. lactis, did not increase the total yield of nisine and did not produce a significant effect on the level or cellular nisine. This indicates an important physiological difference between the culture-nisine producer described by Hirsh and our culture Str. lactis, str. Moscow University.
|
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] |
PMID:21420
|
Effects of neuroleptics on morphine-induced tail erection in mice.
|
Morphine elicits dose-dependent tail erection in mice. Pretreatment of mice with atropine, phenoxybenzamine, propranolol, diphenhydramine, cyproheptadine or parachlorophenylalanine did not interfere with tail erection induced by morphone. Several neuroleptic drugs which are dopamine receptor blocking agents showed a clear antagonistic effect on morphine-induced tail erection (MITE). Haloperidol and penfluridol blocked MITE at doses which only produced a slight behavioral depression. Pimozide and chlorpromazine were less antagonistic than haloperidol and penfluridol and inhibited MITE only at doses which produced a marked behavioral depression. Results indicated that dopamine might be involved in tail erection induced by morphine. MITE in mice might be a useful model for the evaluation of neuroleptic drugs.
|
Effects of neuroleptics on morphine-induced tail erection in mice. Morphine elicits dose-dependent tail erection in mice. Pretreatment of mice with atropine, phenoxybenzamine, propranolol, diphenhydramine, cyproheptadine or parachlorophenylalanine did not interfere with tail erection induced by morphone. Several neuroleptic drugs which are dopamine receptor blocking agents showed a clear antagonistic effect on morphine-induced tail erection (MITE). Haloperidol and penfluridol blocked MITE at doses which only produced a slight behavioral depression. Pimozide and chlorpromazine were less antagonistic than haloperidol and penfluridol and inhibited MITE only at doses which produced a marked behavioral depression. Results indicated that dopamine might be involved in tail erection induced by morphine. MITE in mice might be a useful model for the evaluation of neuroleptic drugs.
|
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] |
PMID:21421
|
Combination operant conditioning--liquid nitrogen immersion chamber for studying neurotransmitter systems and behavior.
|
Studies of neurochemical events associated with behavior require a method of tissue fixation that is rapid and does not itself produce neurochemical changes. An apparatus is described that permits immediate immersion of an unrestrained behaving animal into liquid nitrogen. This method of tissue fixation has the greatest versatility for studying multiple neurotransmitter systems. In addition to the measurement of neurotransmitter content and turnover, investigation of neurotransmitter receptors, enriched nerve ending fractions and enzyme activities are possible. The operant conditioning-liquid nitrogen immersion chamber described here can be used for studying these neurotransmitter systems as they relate to animal's responding on operant schedules of reinforcement.
|
Combination operant conditioning--liquid nitrogen immersion chamber for studying neurotransmitter systems and behavior. Studies of neurochemical events associated with behavior require a method of tissue fixation that is rapid and does not itself produce neurochemical changes. An apparatus is described that permits immediate immersion of an unrestrained behaving animal into liquid nitrogen. This method of tissue fixation has the greatest versatility for studying multiple neurotransmitter systems. In addition to the measurement of neurotransmitter content and turnover, investigation of neurotransmitter receptors, enriched nerve ending fractions and enzyme activities are possible. The operant conditioning-liquid nitrogen immersion chamber described here can be used for studying these neurotransmitter systems as they relate to animal's responding on operant schedules of reinforcement.
|
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] |
PMID:21422
|
Potentiation of beta-sympathomimetics with alpha-adrenoceptor blocking drugs in guinea pig trachea and human bronchus preparations.
|
The actions of beta-sympathomimetics alone and in various combinations with alpha-adrenoceptor blocking agents were studied in guinea pig tracheal chain and in some preparations of human bronchi taken in operations. All the alpha-adrenoceptor blockers caused 50-100% potentiation of the effects of the beta-sympathomimetics studied in both preparations, had no effects of their own in the rather low concentrations used (10(-10) --10(-6) mol/l). The results show that guinea pig and human tracheobronchial smooth muscle react similarly to these drugs and may contain adrenergic alpha-receptors.
|
Potentiation of beta-sympathomimetics with alpha-adrenoceptor blocking drugs in guinea pig trachea and human bronchus preparations. The actions of beta-sympathomimetics alone and in various combinations with alpha-adrenoceptor blocking agents were studied in guinea pig tracheal chain and in some preparations of human bronchi taken in operations. All the alpha-adrenoceptor blockers caused 50-100% potentiation of the effects of the beta-sympathomimetics studied in both preparations, had no effects of their own in the rather low concentrations used (10(-10) --10(-6) mol/l). The results show that guinea pig and human tracheobronchial smooth muscle react similarly to these drugs and may contain adrenergic alpha-receptors.
|
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0.0530250109732151,
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0.020931264385581017,
0.016616297885775566,
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0.027954375371336937,
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0.08543670177459717,
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0.04846841096878052
] |
PMID:21429
|
Norepinephrine-sensitive adenylate cyclase in rat hypothalamus: effects of adrenergic blockers and narcotics.
|
The norepinephrine-sensitive adenylate cyclase system in the rat brain was examined. Adrenergic blocking agents and the relative activity of structurally related catecholamines were employed to determine whether norepinephrine-stimulated accumulation of [3H]c-AMP in the hypothalamus occurred via alpha or beta adrenergic receptors. The results indicate that norepinephrine probably acts through a mixture of alpha and beta receptors in that both alpha and beta adrenergic blockers inhibited norepinephrine-induced accumulation of [3H]c-AMP. Morphine and levorphanol had no significant effect on adenylate cyclase or phosphodiesterase activities in hypothalamic slices or homogenates of several brain regions.
|
Norepinephrine-sensitive adenylate cyclase in rat hypothalamus: effects of adrenergic blockers and narcotics. The norepinephrine-sensitive adenylate cyclase system in the rat brain was examined. Adrenergic blocking agents and the relative activity of structurally related catecholamines were employed to determine whether norepinephrine-stimulated accumulation of [3H]c-AMP in the hypothalamus occurred via alpha or beta adrenergic receptors. The results indicate that norepinephrine probably acts through a mixture of alpha and beta receptors in that both alpha and beta adrenergic blockers inhibited norepinephrine-induced accumulation of [3H]c-AMP. Morphine and levorphanol had no significant effect on adenylate cyclase or phosphodiesterase activities in hypothalamic slices or homogenates of several brain regions.
|
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] |
PMID:21430
|
Determination of 3-methoxy-4-hydroxyphenylglycol in urine and the effect of diet on its excretion.
|
A modified method is described for determination of 3-methoxy-4-hydroxyphenylglycol (MHPG) in urine by gas chromatography with electron capture detection. The method is reproducible and mean (+/- SD) recoveries of MHPG from urine were 78.5 +/- 12.7% and 76.5 +/- 15.0% in two separate series of analyses. Mean 24-hour MHPG excretion was 1884 +/- 591 microgram in 11 normal subjects and 1688 +/- 593 microgram in 20 patients with various types of depression. Males excreted more MHPG than females but this difference could be eliminated by expressing the values relative to the creatinine in urine. Variations in diet did not appear to influence urinary MHPG excretion.
|
Determination of 3-methoxy-4-hydroxyphenylglycol in urine and the effect of diet on its excretion. A modified method is described for determination of 3-methoxy-4-hydroxyphenylglycol (MHPG) in urine by gas chromatography with electron capture detection. The method is reproducible and mean (+/- SD) recoveries of MHPG from urine were 78.5 +/- 12.7% and 76.5 +/- 15.0% in two separate series of analyses. Mean 24-hour MHPG excretion was 1884 +/- 591 microgram in 11 normal subjects and 1688 +/- 593 microgram in 20 patients with various types of depression. Males excreted more MHPG than females but this difference could be eliminated by expressing the values relative to the creatinine in urine. Variations in diet did not appear to influence urinary MHPG excretion.
|
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] |
PMID:21433
|
Properties of blood oxygen transport in the turtle Pseudemys scripta and the tortoise Testudo graeca: effects of temperature, CO2 and pH.
|
Properties of oxygen-haemoglobin binding have been investigated in the aquatic turtle Psuedemys scripta and the terrestrial tortoise Testudo graeca. Haematocrit (30-35%) and haemoglobin concentration (12-14 g/100 ml blood) were similar in both species. P50 at physiological levels of PCO2 (20-25 mm Hg) was 21 mm Hg in Pseudemys, compared with 23 mm Hg in Testudo. The Bohr shift of the blood of both the turtle and the tortoise was almost identical at -0.28. The heat of oxygenation, deltaH, reflecting the temperature sensitivity of O2-Hb affinity, was -10.55 in Pseudemys and -8.12 kcal/mol in Testudo. These data on whole blood do not support previous generalizations in the literature suggesting marked differences in oxygen-haemoglobin binding between aquatic and terrestrial chelonian reptiles.
|
Properties of blood oxygen transport in the turtle Pseudemys scripta and the tortoise Testudo graeca: effects of temperature, CO2 and pH. Properties of oxygen-haemoglobin binding have been investigated in the aquatic turtle Psuedemys scripta and the terrestrial tortoise Testudo graeca. Haematocrit (30-35%) and haemoglobin concentration (12-14 g/100 ml blood) were similar in both species. P50 at physiological levels of PCO2 (20-25 mm Hg) was 21 mm Hg in Pseudemys, compared with 23 mm Hg in Testudo. The Bohr shift of the blood of both the turtle and the tortoise was almost identical at -0.28. The heat of oxygenation, deltaH, reflecting the temperature sensitivity of O2-Hb affinity, was -10.55 in Pseudemys and -8.12 kcal/mol in Testudo. These data on whole blood do not support previous generalizations in the literature suggesting marked differences in oxygen-haemoglobin binding between aquatic and terrestrial chelonian reptiles.
|
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] |
PMID:21434
|
Oxygen affinity of avian blood.
|
Oxygen dissociation curves plotted directly on whole blood during oxygenation using a Radiometer DCA 1 gave P50 values of 39.2 +/- 2.2 mm Hg and 51.3 +/- 6.2 mm Hg for pigeon and chicken blood, respectively, at 41 degrees C, pH 7.5 and PCO2 29 mm Hg. These values agree well with earlier results obtained by a variety of methods; however, they do conflict with recent findings of a much higher oxygen affinity in avian blood which were obtained using a different plotting method. It was shown that with the method used in this paper the high metabolic rate of avian blood has little effect on the plotted curve at saturations below 50%. At higher saturations O2 consumption of red cells affects a progressive shift of the curve to the left so that to obtain accurate curves at high saturation it is necessary to correct the plotted curves for the oxygen utilization.
|
Oxygen affinity of avian blood. Oxygen dissociation curves plotted directly on whole blood during oxygenation using a Radiometer DCA 1 gave P50 values of 39.2 +/- 2.2 mm Hg and 51.3 +/- 6.2 mm Hg for pigeon and chicken blood, respectively, at 41 degrees C, pH 7.5 and PCO2 29 mm Hg. These values agree well with earlier results obtained by a variety of methods; however, they do conflict with recent findings of a much higher oxygen affinity in avian blood which were obtained using a different plotting method. It was shown that with the method used in this paper the high metabolic rate of avian blood has little effect on the plotted curve at saturations below 50%. At higher saturations O2 consumption of red cells affects a progressive shift of the curve to the left so that to obtain accurate curves at high saturation it is necessary to correct the plotted curves for the oxygen utilization.
|
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] |
PMID:21435
|
Gas exchange and acid-base regulation in the blood and extraembryonic fluids of the developing chicken embryo.
|
Measurements of pH, PCO2, PO2 and total CO2 were recorded simultaneously in samples of chorioallantoic fluid, amnionic fluid and blood of the chorioallantoic artery from chicken embryos on days 8, 10, 12, 14, 16, 17 and 18 of incubation. During the incubation period studied, PCO2 levels similarly increased in the blood and extraembryonic fluids. The pH of the blood and amnionic fluid remained approximately constant while the chorioallantoic fluid became progressively acidic. Increases of amnionic fluid and blood HCO-3 indicated that respiartory compensation processes regulate pH. In addition, the disappearance of chorioallantoic fluid HCO-3 suggested that reabsorptive processes may conserve these ions and contribute them to the amnionic fluid by either a direct transfer through the amnioallantoic membrane or by way of the chorioallantoic vascular system.
|
Gas exchange and acid-base regulation in the blood and extraembryonic fluids of the developing chicken embryo. Measurements of pH, PCO2, PO2 and total CO2 were recorded simultaneously in samples of chorioallantoic fluid, amnionic fluid and blood of the chorioallantoic artery from chicken embryos on days 8, 10, 12, 14, 16, 17 and 18 of incubation. During the incubation period studied, PCO2 levels similarly increased in the blood and extraembryonic fluids. The pH of the blood and amnionic fluid remained approximately constant while the chorioallantoic fluid became progressively acidic. Increases of amnionic fluid and blood HCO-3 indicated that respiartory compensation processes regulate pH. In addition, the disappearance of chorioallantoic fluid HCO-3 suggested that reabsorptive processes may conserve these ions and contribute them to the amnionic fluid by either a direct transfer through the amnioallantoic membrane or by way of the chorioallantoic vascular system.
|
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] |
PMID:21443
|
Relationship between gastro-oesophageal acid reflux, basal gastro-oesophageal sphincter pressure, and gastric acid secretion.
|
Twelve-hour continuous pH-recording at the distal end of the oesophagus and measurement of basal gastro-oesophageal sphincter pressure with perfused catheters were carried out in 108 subjects. Fasting gastric secretion, basal secretion, and maximal acid secretion after subcutaneous injection of 6 microgram pentagastrin/kg bodyweight were determined additionally in some of the subjects. There was a significant inverse correlation between the results of continuous pH-recording and basal gastro-oesophageal sphincter pressure, which confirms the relationship between low sphincter pressure and gastro-oesophageal acid reflux. Furthermore, there was a significant direct correlation between the results of continuous pH-recording and the volume of basal secretion and the basal acid output. These findings emphasize the significance of gastric acid secretion for the results of continuous pH-recording. As reflux-preventive surgery may elicit alterations in the variables of acid secretion, the results of continuous pH-recording do not allow conclusions to be drawn with regard to the effectiveness of a surgically established gastro-oesophageal barrier.
|
Relationship between gastro-oesophageal acid reflux, basal gastro-oesophageal sphincter pressure, and gastric acid secretion. Twelve-hour continuous pH-recording at the distal end of the oesophagus and measurement of basal gastro-oesophageal sphincter pressure with perfused catheters were carried out in 108 subjects. Fasting gastric secretion, basal secretion, and maximal acid secretion after subcutaneous injection of 6 microgram pentagastrin/kg bodyweight were determined additionally in some of the subjects. There was a significant inverse correlation between the results of continuous pH-recording and basal gastro-oesophageal sphincter pressure, which confirms the relationship between low sphincter pressure and gastro-oesophageal acid reflux. Furthermore, there was a significant direct correlation between the results of continuous pH-recording and the volume of basal secretion and the basal acid output. These findings emphasize the significance of gastric acid secretion for the results of continuous pH-recording. As reflux-preventive surgery may elicit alterations in the variables of acid secretion, the results of continuous pH-recording do not allow conclusions to be drawn with regard to the effectiveness of a surgically established gastro-oesophageal barrier.
|
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0.006367294583469629,
-0.06658796966075897,
0.013769338838756084,
0.020579803735017776,
0.011784715577960014,
0.026751115918159485,
-0.02244464121758938,
0.05871092155575752,
0.05692702904343605
] |
PMID:21444
|
Gastro-oesophageal acid reflux in patients with symptomatic hiatus hernia and effect of a modified Belsey MK IV repair on acid reflux.
|
Twelve-hour continuous recording of pH at the distal end of the oesophagus was carried out in 59 patients with sliding hiatus hernia and symptoms suggestive of gastro-oesophageal reflux, and the results were compared with those obtained in normal subjects. Mean duration of pH less than or equal to 2.3, pH less than or equal to 3, pH less than or equal to 4 and pH less than or equal to 5, expressed in percentages of the total time of recording, was longer in patients than in normal subjects. There was no difference in mean number of reflux episodes between patients and normal subjects. The clearest separation between the two groups was obtained by the variable 'duration of pH less than or equal to 5'. Irrespective of the variable used, the results did not seem to be related to the degree of severity of the symptoms. Individual sensitivity of the oesophageal mucosa, the content of bilious components in the refluxed material, and the semi-quantitative character of the investigation may, in part, account for the results. Furthermore, the same investigation was carried out before and three months after a modified Belsey MK IV repair in 39 patients with hiatus hernia and symptoms indicating surgical treatment. The operation was followed by a reduction in the tendency to acid reflux, probably as a result of an increase in the competence of the gastro-oesophageal region.
|
Gastro-oesophageal acid reflux in patients with symptomatic hiatus hernia and effect of a modified Belsey MK IV repair on acid reflux. Twelve-hour continuous recording of pH at the distal end of the oesophagus was carried out in 59 patients with sliding hiatus hernia and symptoms suggestive of gastro-oesophageal reflux, and the results were compared with those obtained in normal subjects. Mean duration of pH less than or equal to 2.3, pH less than or equal to 3, pH less than or equal to 4 and pH less than or equal to 5, expressed in percentages of the total time of recording, was longer in patients than in normal subjects. There was no difference in mean number of reflux episodes between patients and normal subjects. The clearest separation between the two groups was obtained by the variable 'duration of pH less than or equal to 5'. Irrespective of the variable used, the results did not seem to be related to the degree of severity of the symptoms. Individual sensitivity of the oesophageal mucosa, the content of bilious components in the refluxed material, and the semi-quantitative character of the investigation may, in part, account for the results. Furthermore, the same investigation was carried out before and three months after a modified Belsey MK IV repair in 39 patients with hiatus hernia and symptoms indicating surgical treatment. The operation was followed by a reduction in the tendency to acid reflux, probably as a result of an increase in the competence of the gastro-oesophageal region.
|
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] |
PMID:21446
|
Anti-parental lymphocyte reactions in neonatal F1 hybrid rats.
|
The subpopulation of parental-strain lymphocytes responsible for the recognition of a particular F1 hybrid strain as foreign has been shown to be subject to specific, reversible inactivation after its injection into neonatal rats of that F1 hybrid strain. Neonates born to mothers that were syngeneic with the parental-strain lymphocytes under test acquired the capacity to inactivate these lymphocytes at an earlier age than did the genotypically identical reciprocal F1 hybrids. Neonates had little capacity to inactivate completely allogeneic lymphocytes. It is inferred from the difference in behavior between reciprocal F1 hybrids that the augmented ability to inactivate anti-F1 hybrid maternal-strain lymphocytes follows exposure to such cells in utero and to antibodies with anti-F1 hybrid activity in colostrum. Specific inactivation of those marauding maternal lymphocytes with anti-fetal activity is envisaged as an important means of protection of the fetus from immunological attack by the mother. On the basis of the results presented in this and the preceding paper, it has been proposed that many of the sequelae of the transfer of immunocompetent parental-strain cells to F1 hybrid animals result not from graft anti-host activity but from an F1 hybrid anti-parental lymphocyte response that has eluded normal regulatory mechanisms. These experiments also raise the possibility that regulation of auto-immune responses may be achieved by the inactivation of lymphocytes with anti-self reactivity by other lymphocytes that respond to the recognition structure required for such reactivity.
|
Anti-parental lymphocyte reactions in neonatal F1 hybrid rats. The subpopulation of parental-strain lymphocytes responsible for the recognition of a particular F1 hybrid strain as foreign has been shown to be subject to specific, reversible inactivation after its injection into neonatal rats of that F1 hybrid strain. Neonates born to mothers that were syngeneic with the parental-strain lymphocytes under test acquired the capacity to inactivate these lymphocytes at an earlier age than did the genotypically identical reciprocal F1 hybrids. Neonates had little capacity to inactivate completely allogeneic lymphocytes. It is inferred from the difference in behavior between reciprocal F1 hybrids that the augmented ability to inactivate anti-F1 hybrid maternal-strain lymphocytes follows exposure to such cells in utero and to antibodies with anti-F1 hybrid activity in colostrum. Specific inactivation of those marauding maternal lymphocytes with anti-fetal activity is envisaged as an important means of protection of the fetus from immunological attack by the mother. On the basis of the results presented in this and the preceding paper, it has been proposed that many of the sequelae of the transfer of immunocompetent parental-strain cells to F1 hybrid animals result not from graft anti-host activity but from an F1 hybrid anti-parental lymphocyte response that has eluded normal regulatory mechanisms. These experiments also raise the possibility that regulation of auto-immune responses may be achieved by the inactivation of lymphocytes with anti-self reactivity by other lymphocytes that respond to the recognition structure required for such reactivity.
|
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] |
PMID:21448
|
Sensitization of contracted tracheal smooth muscle to beta-adrenergic spasmolysis by subthreshold doses of papaverine.
|
In certain cases beta-adrenergic substances cause little or no relaxation of tracheal or bronchiolar smooth muscles contracted by spasmogenic mediators. This phenomenon is explained on the basis of the model of functional antagonism, with the suppositions that the spasmogenic system has a reserve and the spasmogen concentrations are much higher than the concentration which would cause a just-maximal contraction. If this is correct, the model predicts that it should be possible to restore the effectiveness of the beta-adrenergic spasmolytics with low doses of a non-competitive (metactoid) spasmolytic, provided that this substance acts by depressing the subeffect curve. Such a metactoid antagonist should cause the desired result in subthreshold concentrations, i.e. concentrations which as such do not cause relaxation of the contracted muscles. In a series of experiments on the isolated tracheal chain of the guinea-pig the results agreed with this expectation. This provides additional proof for the model of functional interaction and suggests that the combination of beta-adrenergics with low doses of a metactoid spasmolytic may be of clinical interest.
|
Sensitization of contracted tracheal smooth muscle to beta-adrenergic spasmolysis by subthreshold doses of papaverine. In certain cases beta-adrenergic substances cause little or no relaxation of tracheal or bronchiolar smooth muscles contracted by spasmogenic mediators. This phenomenon is explained on the basis of the model of functional antagonism, with the suppositions that the spasmogenic system has a reserve and the spasmogen concentrations are much higher than the concentration which would cause a just-maximal contraction. If this is correct, the model predicts that it should be possible to restore the effectiveness of the beta-adrenergic spasmolytics with low doses of a non-competitive (metactoid) spasmolytic, provided that this substance acts by depressing the subeffect curve. Such a metactoid antagonist should cause the desired result in subthreshold concentrations, i.e. concentrations which as such do not cause relaxation of the contracted muscles. In a series of experiments on the isolated tracheal chain of the guinea-pig the results agreed with this expectation. This provides additional proof for the model of functional interaction and suggests that the combination of beta-adrenergics with low doses of a metactoid spasmolytic may be of clinical interest.
|
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] |
PMID:21449
|
[Intermittent positive pressure breathing (IPPB) with respirators in home nursing].
|
29 patients using a home respirator have been studied. Management of the respirator and inhalation were correct in 86%. Bacteriologic contamination in home treatment poses few problems. Blood gases and spirometric lung function tests do not demonstrate amelioration but show stabilization in long term treatment. Costs are high. Nevertheless, this treatment is indicated in certain carefully selected patients. Follow-up checks are essential.
|
[Intermittent positive pressure breathing (IPPB) with respirators in home nursing]. 29 patients using a home respirator have been studied. Management of the respirator and inhalation were correct in 86%. Bacteriologic contamination in home treatment poses few problems. Blood gases and spirometric lung function tests do not demonstrate amelioration but show stabilization in long term treatment. Costs are high. Nevertheless, this treatment is indicated in certain carefully selected patients. Follow-up checks are essential.
|
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] |
PMID:21451
|
The white cloud. The changing pattern of hematologic research as exemplified by studies of oxygen transport.
|
Medical research has become an integral part of governmental health care systems. As a consequence of this subsidization, its resources are far greater, while its activities have become more directly responsible to the perceived needs of the people. Clinical investigation in particular has been affected by this adjustment, and its decreasing role in the total program needs scrutiny. Progress in our understanding of oxygen transport is reviewed as an example of the capacity of today's scientific community to explore and develop new areas of knowledge.
|
The white cloud. The changing pattern of hematologic research as exemplified by studies of oxygen transport. Medical research has become an integral part of governmental health care systems. As a consequence of this subsidization, its resources are far greater, while its activities have become more directly responsible to the perceived needs of the people. Clinical investigation in particular has been affected by this adjustment, and its decreasing role in the total program needs scrutiny. Progress in our understanding of oxygen transport is reviewed as an example of the capacity of today's scientific community to explore and develop new areas of knowledge.
|
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] |
PMID:21452
|
Deuterolysis of amino acid precursors: evidence for hydrogen cyanide polymers as protein ancestors.
|
Deuterolysis experiments suggest that hydrogen cyanide polymers rather than aminoacetonitriles are major precursors of alpha-amino acids obtained from spark reactions and other studies on chemical evolution. These results are consistent with the hypothesis that the original heteropolypeptides on the earth were synthesized spontaneously from hydrogen cyanide and water without the intervening formation of alpha-amino acids.
|
Deuterolysis of amino acid precursors: evidence for hydrogen cyanide polymers as protein ancestors. Deuterolysis experiments suggest that hydrogen cyanide polymers rather than aminoacetonitriles are major precursors of alpha-amino acids obtained from spark reactions and other studies on chemical evolution. These results are consistent with the hypothesis that the original heteropolypeptides on the earth were synthesized spontaneously from hydrogen cyanide and water without the intervening formation of alpha-amino acids.
|
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] |
PMID:21453
|
Flurazepam effects on slow-wave sleep: stage 4 suppressed but number of delta waves constant.
|
Repeated administration of flurazepam reduced stage 4 sleep (high delta-wave concentration) but produced a greater increase in stage 2 duration so that total sleep time was increased. Computer analysis revealed that the increased amount of stage 2 (low delta-wave concentration) sleep provided a number and duration of delta waves sufficient to offset the loss of delta activity in stage 4. However, the amplitude of the average delta wave was reduced. These results demonstrate the value of direct quantification of delta-wave activity, the variable that underlies visual classification of slow-wave sleep into stages 2 to 4. They also give rise to new hypotheses regarding the relative absence of side effects in spite of profound stage 4 suppression by flurazepam and the mechanisms by which total sleep time is increased by this drug.
|
Flurazepam effects on slow-wave sleep: stage 4 suppressed but number of delta waves constant. Repeated administration of flurazepam reduced stage 4 sleep (high delta-wave concentration) but produced a greater increase in stage 2 duration so that total sleep time was increased. Computer analysis revealed that the increased amount of stage 2 (low delta-wave concentration) sleep provided a number and duration of delta waves sufficient to offset the loss of delta activity in stage 4. However, the amplitude of the average delta wave was reduced. These results demonstrate the value of direct quantification of delta-wave activity, the variable that underlies visual classification of slow-wave sleep into stages 2 to 4. They also give rise to new hypotheses regarding the relative absence of side effects in spite of profound stage 4 suppression by flurazepam and the mechanisms by which total sleep time is increased by this drug.
|
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] |
PMID:21455
|
Repeat myocardial revascularization for uncontrollable angina after occlusion of prior aortocoronary bypass.
|
Twelve patients at Emory University Hospital have had repeat myocardial revascularization for recurrent, uncontrollable, disabling angina pectoris after previous coronary artery bypass grafts. The interval betweeen initial bypass procedure and reoperation ranged from six weeks to six years. The native coronary circulation remained unchanged in six, had developed additional proximal (left main) obstruction in four, and had advanced stenosis at the site of former anastomosis in three. Repeat revascularization consisted of new vein graft construction in eight and vein and internal mammary artery graft in four, with an average of 1.9 grafts per patient. There were no deaths. Seven of 12 patients (60%) are now asymptomatic and three of 12 (25%) are significantly improved. Patency of new grafts studied by elective repeat coronary angiography in six patients showed patency of all grafts to the left anterior descending artery and four of six grafts to other vessels. Analysis of the initial graft closures, method for selecting patients to undergo a second procedure, and operative technics believed important in safety of reoperation and avoidance of repeat early graft occlusion are presented.
|
Repeat myocardial revascularization for uncontrollable angina after occlusion of prior aortocoronary bypass. Twelve patients at Emory University Hospital have had repeat myocardial revascularization for recurrent, uncontrollable, disabling angina pectoris after previous coronary artery bypass grafts. The interval betweeen initial bypass procedure and reoperation ranged from six weeks to six years. The native coronary circulation remained unchanged in six, had developed additional proximal (left main) obstruction in four, and had advanced stenosis at the site of former anastomosis in three. Repeat revascularization consisted of new vein graft construction in eight and vein and internal mammary artery graft in four, with an average of 1.9 grafts per patient. There were no deaths. Seven of 12 patients (60%) are now asymptomatic and three of 12 (25%) are significantly improved. Patency of new grafts studied by elective repeat coronary angiography in six patients showed patency of all grafts to the left anterior descending artery and four of six grafts to other vessels. Analysis of the initial graft closures, method for selecting patients to undergo a second procedure, and operative technics believed important in safety of reoperation and avoidance of repeat early graft occlusion are presented.
|
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] |
PMID:21457
|
Minocycline treatment failure in pneumonia caused by minocycline-sensitive Streptococcus pneumoniae.
|
A previously healthy 23-year-old white woman had fulminant pneumococcal pneumonia complicated by empyema and bilateral pneumothoraces. Despite early treatment with the recommended doses of minocycline, the disease progressed. The S pneumoniae isolate was resistant to a 30microgram tetracycline disk and showed an MIC of 3.13microgram/ml for minocycline and 12.5 microgram/ml for tetracycline; these levels are considered by the manufacturer to indicate sensitivity to minocycline and intermediate sensitivity to tetracycline. The tetracyclines, including minocycline, should not be used to treat bacterial pneumonia since resistant strains of pneumococci are not uncommon and inffective treatment can lead to rapid progression of the infection. This case suggests that the levels of minocycline considered to indicate sensitivity in vitro be reassessed.
|
Minocycline treatment failure in pneumonia caused by minocycline-sensitive Streptococcus pneumoniae. A previously healthy 23-year-old white woman had fulminant pneumococcal pneumonia complicated by empyema and bilateral pneumothoraces. Despite early treatment with the recommended doses of minocycline, the disease progressed. The S pneumoniae isolate was resistant to a 30microgram tetracycline disk and showed an MIC of 3.13microgram/ml for minocycline and 12.5 microgram/ml for tetracycline; these levels are considered by the manufacturer to indicate sensitivity to minocycline and intermediate sensitivity to tetracycline. The tetracyclines, including minocycline, should not be used to treat bacterial pneumonia since resistant strains of pneumococci are not uncommon and inffective treatment can lead to rapid progression of the infection. This case suggests that the levels of minocycline considered to indicate sensitivity in vitro be reassessed.
|
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] |
PMID:21458
|
Observation on the reduction of the prevalence of malayan filariasis in Chumphon Province of South Thailand.
|
Further studies on malayan filariasis were made at Bangluke canton of Chumphon province of South Thailand, where mass drug treatment was not applied. It was found after 9 years that there was a marked reduction in filariasis in the area. The filariasis infection rate being decreased from 14.1 to 1.9 per cent, the microfilarial rate from 10.8 to 0.9 per cent, and the elephantiasis rate from 3.3 to 1.0 per cent, and the mean microfilarial density among positive cases being decreased from 27.6 to 6.6 per 20 c.mm blood. Dissection of 1,893 Mansonia mosquitoes revealed the finding of only stage I and stage II larvae of B. malayi in seven M. annulifera and M. indiana. The reduction in the filariasis infection was assumed to be due to the interruption of transmission of filariasis cycle in the mosquitoes resulting from DDT spraying operation of the Malaria Eradication Programme of the Thai Government. There were also some positive cases moving out of the area. The rural development programme of the Thai Government also played another important role in the reduction in the prevalence of malayan filariasis in this area.
|
Observation on the reduction of the prevalence of malayan filariasis in Chumphon Province of South Thailand. Further studies on malayan filariasis were made at Bangluke canton of Chumphon province of South Thailand, where mass drug treatment was not applied. It was found after 9 years that there was a marked reduction in filariasis in the area. The filariasis infection rate being decreased from 14.1 to 1.9 per cent, the microfilarial rate from 10.8 to 0.9 per cent, and the elephantiasis rate from 3.3 to 1.0 per cent, and the mean microfilarial density among positive cases being decreased from 27.6 to 6.6 per 20 c.mm blood. Dissection of 1,893 Mansonia mosquitoes revealed the finding of only stage I and stage II larvae of B. malayi in seven M. annulifera and M. indiana. The reduction in the filariasis infection was assumed to be due to the interruption of transmission of filariasis cycle in the mosquitoes resulting from DDT spraying operation of the Malaria Eradication Programme of the Thai Government. There were also some positive cases moving out of the area. The rural development programme of the Thai Government also played another important role in the reduction in the prevalence of malayan filariasis in this area.
|
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] |
PMID:21459
|
Anaesthetic induction and maintenance with flunitrazepam.
|
Flunitrazepam (Rohypnol) was investigated as an intravenous induction agent for dental procedures in 15 patients in a private anaesthetic practice. During this study it was noted that the normal halothane requirement could be reduced substantially. A second study to investigate this new phenomenon was done on 50 patients who underwent major surgery. The results indicate that adequate anaesthesia can be maintained with flunitrazepam.
|
Anaesthetic induction and maintenance with flunitrazepam. Flunitrazepam (Rohypnol) was investigated as an intravenous induction agent for dental procedures in 15 patients in a private anaesthetic practice. During this study it was noted that the normal halothane requirement could be reduced substantially. A second study to investigate this new phenomenon was done on 50 patients who underwent major surgery. The results indicate that adequate anaesthesia can be maintained with flunitrazepam.
|
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] |
PMID:21461
|
Blood viscosity in modern medicine.
|
The understanding and measurement of blood viscosity play an important part in mordern medicine. The basic principles and relevances of fluid viscosity are discussed. Factors which alter viscosity include shear rate, haematocrit, erythrocyte deformability, internal fluidity, pH, plasma proteins, temperature, osmolality, lipids and leucocytes. In vivo changes in vascular architecture are thought to influence blood viscosity. Some of the clinical conditions in which viscosity is important are described. Hyperviscosity should be treated before complications arise.
|
Blood viscosity in modern medicine. The understanding and measurement of blood viscosity play an important part in mordern medicine. The basic principles and relevances of fluid viscosity are discussed. Factors which alter viscosity include shear rate, haematocrit, erythrocyte deformability, internal fluidity, pH, plasma proteins, temperature, osmolality, lipids and leucocytes. In vivo changes in vascular architecture are thought to influence blood viscosity. Some of the clinical conditions in which viscosity is important are described. Hyperviscosity should be treated before complications arise.
|
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] |
PMID:21462
|
Fertility in undescended testes.
|
Since 1956 many children with undescended testes have been treated at the Red Cross War Memorial Children's Hospital in Cape Town, and in this article the conesequent degree of fertility achieved by orchidopexy, the method of treatment, is appraised. In 567 children the condition was unilateral, and in 202 it was bilateral. Assessment of potential fertility in 76 unilateral and in 29 bilateral cases was mainly by semen analysis; the average age of the youths at the time of the examination was 19 years, and parenthood was therefore regarded as an unsuitable criterion for assessment. Four hundred and ninety-two youths had their condition reviewed, and the condition of 587 testes was assessed. The anatomical state of the testes was ascertained to help in the assessment, but also, and of greater importance, to obtain evidence of the usefulness of orchidopexy for cosmetic or psychological benefit. Biopsy of the affected testes, carried out in some, proved to be nor more informative than the anatomical appraisal, with regard to spermatogenesis. Two useful facts emerged from the study. About 10% of bilateral undescended testes are capable of normal spermatogenesis after orchidopexy, and 65% are sterile, while the fertility of persons with unilateral undescended testis is impaired, 28% having little hope of paternity, and 4% no hope at all.
|
Fertility in undescended testes. Since 1956 many children with undescended testes have been treated at the Red Cross War Memorial Children's Hospital in Cape Town, and in this article the conesequent degree of fertility achieved by orchidopexy, the method of treatment, is appraised. In 567 children the condition was unilateral, and in 202 it was bilateral. Assessment of potential fertility in 76 unilateral and in 29 bilateral cases was mainly by semen analysis; the average age of the youths at the time of the examination was 19 years, and parenthood was therefore regarded as an unsuitable criterion for assessment. Four hundred and ninety-two youths had their condition reviewed, and the condition of 587 testes was assessed. The anatomical state of the testes was ascertained to help in the assessment, but also, and of greater importance, to obtain evidence of the usefulness of orchidopexy for cosmetic or psychological benefit. Biopsy of the affected testes, carried out in some, proved to be nor more informative than the anatomical appraisal, with regard to spermatogenesis. Two useful facts emerged from the study. About 10% of bilateral undescended testes are capable of normal spermatogenesis after orchidopexy, and 65% are sterile, while the fertility of persons with unilateral undescended testis is impaired, 28% having little hope of paternity, and 4% no hope at all.
|
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] |
PMID:21463
|
Biochemical genetic analysis of pyrimidine biosynthesis in mammalian cells: I. Isolation of a mutant defective in the early steps of de novo pyrimidine synthesis.
|
The isolation and characterization of a new mutant of Chinese hamster ovary cells is described. This mutant, Urd-A, shows an absolute requirement for exogenously added pyrimidines for growth. Complementation analysis indicates that the lesion in this mutant is recessive. Revertants can be isolated at frequencies suggesting that it is a single gene alteration. Biochemical analysis of cell-free extracts of CHO-K1 (Urd+) and Urd-A revealed that Urd-A possesses no more than 10% of wild-type levels of carbamyl phosphate synthetase (EC 2.7.2.9) activity, no more than 1% of wild-type levels of aspartate transcarbamylase (EC 1.2.3.2) activity, and undetectable levels of dihydroorotase (EC 3.5.2.3) activity. Thus, this mutant appears simultaneously to possess marked or complete deficiencies in the activities of the first three enzymes of pyrimidine biosynthesis. Activities of the other enzymes of the pathway appear normal. The use of this mutant for biochemical-genetic studies of pyrimidine biosynthesis is discussed.
|
Biochemical genetic analysis of pyrimidine biosynthesis in mammalian cells: I. Isolation of a mutant defective in the early steps of de novo pyrimidine synthesis. The isolation and characterization of a new mutant of Chinese hamster ovary cells is described. This mutant, Urd-A, shows an absolute requirement for exogenously added pyrimidines for growth. Complementation analysis indicates that the lesion in this mutant is recessive. Revertants can be isolated at frequencies suggesting that it is a single gene alteration. Biochemical analysis of cell-free extracts of CHO-K1 (Urd+) and Urd-A revealed that Urd-A possesses no more than 10% of wild-type levels of carbamyl phosphate synthetase (EC 2.7.2.9) activity, no more than 1% of wild-type levels of aspartate transcarbamylase (EC 1.2.3.2) activity, and undetectable levels of dihydroorotase (EC 3.5.2.3) activity. Thus, this mutant appears simultaneously to possess marked or complete deficiencies in the activities of the first three enzymes of pyrimidine biosynthesis. Activities of the other enzymes of the pathway appear normal. The use of this mutant for biochemical-genetic studies of pyrimidine biosynthesis is discussed.
|
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] |
PMID:21467
|
[Veterinary and clinical experience of the use of a beta2-receptor-stimulating sympathicomimetic agent (NAB 365) in horses with respiratory discase (author's transl)].
|
The manufacturers state that NAB 365 is a beta2-receptor-stimulating sympathicomimetic agent. According to the medical literature it combines a bronchial antispasmodic effect with certain bronchia secretolytic properties and has few untoward side-effects on, for instance, the heart and intestine. The effectiveness of administration of NAB 365 in horses with chronic or acute respiratory disease was tested in the Department of Veterinary Internal medicine in Utrecht. NAB 365 administered at a dosage of 0.8 gamma/kg, of body weight was found to have a marked bronchodilative effect in horses. There was also evidence of a bronchialsecretolytic effect. NAB 365 has a beneficial effect on respiration. At a dosage of 0.8 gamma/kg of body weight, twice daily, there are few side-effects, even when administration is continued for a fortnight. The clinical effect on respiration continued practically throughout the day.
|
[Veterinary and clinical experience of the use of a beta2-receptor-stimulating sympathicomimetic agent (NAB 365) in horses with respiratory discase (author's transl)]. The manufacturers state that NAB 365 is a beta2-receptor-stimulating sympathicomimetic agent. According to the medical literature it combines a bronchial antispasmodic effect with certain bronchia secretolytic properties and has few untoward side-effects on, for instance, the heart and intestine. The effectiveness of administration of NAB 365 in horses with chronic or acute respiratory disease was tested in the Department of Veterinary Internal medicine in Utrecht. NAB 365 administered at a dosage of 0.8 gamma/kg, of body weight was found to have a marked bronchodilative effect in horses. There was also evidence of a bronchialsecretolytic effect. NAB 365 has a beneficial effect on respiration. At a dosage of 0.8 gamma/kg of body weight, twice daily, there are few side-effects, even when administration is continued for a fortnight. The clinical effect on respiration continued practically throughout the day.
|
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-0.041041646152734756,
0.07723703235387802,
0.080796018242836
] |
PMID:21469
|
Antibacterial activity detected in duodenal juice.
|
Antibacterial activity could be detected in bacterium-negative duodenal juice from 3 patients, whereas it was not detected in bacterium-positive duodenal juice from other 3 patients. The follow-up study revealed that appearance of the activity in duodenal juice was just coincident with disappearance of bacteria in duodenal juice. The activity was not influenced by pH of the duodenal juice. These results seem to suggest that some antibacterial activity, different from that of pH, in duodenal juice regulates in some way proliferation of the upper gastrointestinal flora.
|
Antibacterial activity detected in duodenal juice. Antibacterial activity could be detected in bacterium-negative duodenal juice from 3 patients, whereas it was not detected in bacterium-positive duodenal juice from other 3 patients. The follow-up study revealed that appearance of the activity in duodenal juice was just coincident with disappearance of bacteria in duodenal juice. The activity was not influenced by pH of the duodenal juice. These results seem to suggest that some antibacterial activity, different from that of pH, in duodenal juice regulates in some way proliferation of the upper gastrointestinal flora.
|
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] |
PMID:21470
|
A rapid fluorometric assay of angiotensin-converting enzyme.
|
A rapid, simple and sensitive method is described for the fluorometric assay of angiotesin-converting enzyme using Fluorescamine. The critical factors such as optimal pH, incubation time, chloride ion, and inactivation by EDTA and 8-hydroxyquinoline were examined. The Km value for hippuryl-L-histidyl-L-leucine was 0.5 mM. This method was applied to the assay of angiotensin-converting enzyme in the rat serum and the reproducible values were obtained with a 10 mul of the rat serum.
|
A rapid fluorometric assay of angiotensin-converting enzyme. A rapid, simple and sensitive method is described for the fluorometric assay of angiotesin-converting enzyme using Fluorescamine. The critical factors such as optimal pH, incubation time, chloride ion, and inactivation by EDTA and 8-hydroxyquinoline were examined. The Km value for hippuryl-L-histidyl-L-leucine was 0.5 mM. This method was applied to the assay of angiotensin-converting enzyme in the rat serum and the reproducible values were obtained with a 10 mul of the rat serum.
|
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] |
PMID:21471
|
Methylmalonyl-CoA mutase activity of leukocytes in variants and heterozygotes of methylmalonic acidemia.
|
An assay method for the methylmalonyl-CoA mutase of leukocytes obtained from 3 ml of blood was established. The enzyme activity which was measured with or without the in vitro addition of 5'-deoxyadenosylcobalamin was found to be of value for the diagnosis of two variants of methylmalonic acidemia (vitamin B12 responsive and unresponsive), and also for the detection of heterozygotes with the vitamin B12 unresponsive type.
|
Methylmalonyl-CoA mutase activity of leukocytes in variants and heterozygotes of methylmalonic acidemia. An assay method for the methylmalonyl-CoA mutase of leukocytes obtained from 3 ml of blood was established. The enzyme activity which was measured with or without the in vitro addition of 5'-deoxyadenosylcobalamin was found to be of value for the diagnosis of two variants of methylmalonic acidemia (vitamin B12 responsive and unresponsive), and also for the detection of heterozygotes with the vitamin B12 unresponsive type.
|
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] |
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