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ecab97a7-a0bb-4313-a8bf-c565e3bd3df5
| 0 |
Effect of tobramycin on urinary gamma-glutamyltransferase activity: Studies in a case of renal carcinoma. Gamma-Glutamyltransferase activity was studied in a man presenting with recurrent septicemia owing to pyonephrosis and renal carcinoma. Increased activity in the urine was ascribable to administration of the aminoglycoside antibiotic, tobramycin. That the renal carcinoma did not contribute to the increased values was confirmed by homogenization and enzyme histochemistry of the tumor. Although the activity of this enzyme in serum was greater than normal, this persisted postoperatively, and thus was not related to the renal carcinoma.
|
9b1dc2d0-260a-48e2-95ac-4ba4f1af117d
| 0 |
Electrophoresis of gamma-glutamyltranspeptidase on cellogel. The appearance of the alpha2-beta band in positive LP-X sera. Fractionations of serum gamma-glutamyltranspeptidase (gamma-GT) and determinations of the "abnormal serum lipoprotein X" (LP-X) have been carried out in sera from patients with different hepatobiliary disorders. LP-X was used to demonstrate or exclude cholestasis. One gamma-GT fraction, alpha2-beta, may be of interest to distinguish between extrahepatic obstruction and intrahepatic cholestasis as was revealed by statistical analysis.
|
190f7a38-7818-4761-ada8-3dbe7918578a
| 0 |
Multiple changes in distal stop-flow electrolyte patterns and reduction of acid excretion induced in rabbits by angiotensin. 1. Angiotensin has previously been shown to inhibit distal renal tubular sodium reabsorption. As a consequence of this, or independently, it might influence the distal handling of other electrolytes. We have therefore examined the effects of angiotensin on the distal reabsorption or secretion of a spectrum of electrolytes.
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190f7a38-7818-4761-ada8-3dbe7918578a
| 1 |
2. Standard bilateral stop-flow studies were done on anaesthetized, adrenalectomized rabbits, in which the effects of intravenous infusions of either 0-02-0-05 mug min-1 kg-1 or 1 mug min-1 kg-1 of angiotensin were compared with control stop-flow results. 3. The lower dose of angiotensin inhibited distal sodium, chloride, water and magnesium reabsorption, inhibited distal hydrogen secretion and stimulated distal potassium secretion.
|
190f7a38-7818-4761-ada8-3dbe7918578a
| 2 |
The higher dose of angiotensin produced these changes and additionally inhibited distal calcium reabsorption. Most of the observed changes were dose-related. The low dose of angiotensin did not significantly raise blood pressure but the high dose was pressor. 4. Changes in the stop-flow patterns induced by the higher dose of angiotensin were compatible with, and may help to explain, the changes it produced in urinary excretion of sodium, chloride, potassium, magnesium and calcium in clearance studies before stop-flow.
|
190f7a38-7818-4761-ada8-3dbe7918578a
| 3 |
Suppression of hydrogen secretion caused by both doses of angiotensin in the stop-flow studies was also reflected by reductions in acid excretion produced by these infusion rates in additional experiments performed by clearance methods in acid-loaded, conscious rabbits. 5. The results support the view that angiotensin may have an important intrarenal role, at least in rabbits.
|
537926c1-40b8-4455-ac8d-200e3585604b
| 0 |
The acute effects of respiratory and metabolic acidosis on renal function in the dog. 1. Effective renal plasma flow, glomerular filtration rate and cardiac output were measured in osmotically loaded dogs before and during comparable acute respiratory and metabolic acidosis. 2. Urine output increased in control dogs and in animals with metabolic acidosis, but declined with respiratory acidosis.
|
537926c1-40b8-4455-ac8d-200e3585604b
| 1 |
Effective renal plasma flow and glomerular filtration rate declined with respiratory and metabolic acidosis. 3. When respiratory acidosis was buffered with sodium bicarbonate, urine volume increased and glomerular filtration rate and effective renal plasma flow were unchanged; with trihydroxymethylaminomethane, urine volume increased but glomerular filtration rate and effective renal plasma flow fell.
|
537926c1-40b8-4455-ac8d-200e3585604b
| 2 |
4. When metabolic acidosis was buffered with sodium bicarbonate, urine volume increased; with trihydroxymethylaminomethane, urine volume increased but glomerular filtration rate fell. Cardiac output declined only during metabolic acidosis, both buffered and unbuffered. 5. These studies demonstrate that, even with osmotic loading: (1) respiratory acidosis caused a decrease in glomerular filtration rate, effective renal plasma flow and urine volume;
|
537926c1-40b8-4455-ac8d-200e3585604b
| 3 |
(2) metabolic acidosis depresses glomerular filtration rate and effective renal plasma flow but does not change urine volume even though cardiac output falls; (3) sodium bicarbonate is mor effective than trihydroxymethylaminomethane in preserving renal function during respiratory and metabolic acidosis.
|
462d3262-12b9-44ad-80c2-235ca8fcec92
| 0 |
The haemodynamic effects of metabolic acidosis in the rat. 1. The effect of metabolic acidosis of 4-6 h duration on cardiac output, blood pressure, heart rate, and hepatic and renal blood flow has been studied in the rat. 2. In anaesthetized rats, blood pressure and heart rate fell linearly with blood pH in both sham-operated and nephrectomized rats.
|
462d3262-12b9-44ad-80c2-235ca8fcec92
| 1 |
There was no significant difference between the two groups in the effect of acidosis on either variable. 3. Cardiac output showed a significant fall with increasing acidosis in the conscious rat. 4. Estimated hepatic blood flow in conscious rats showed a significant positive correlation with blood pH in both sham-operated and nephrectomized animals.
|
462d3262-12b9-44ad-80c2-235ca8fcec92
| 2 |
There was no significant difference in estimated hepatic blood flow between the two groups of animals at any blood pH. 5. In conscious rats, increasing acidosis caused a progressive decrease in estimated renal blood flow. 6. It is concluded that the increase in the previously described apparent renal contribution to lactate removal in the acidotic rat cannot be explained by any circulatory effect mediated by the kidney.
|
462d3262-12b9-44ad-80c2-235ca8fcec92
| 3 |
The possible relevance of the findings to lactate homeostasis is discussed.
|
7e138e7d-198d-4862-8d76-93e0fe251c93
| 0 |
The effect of acidosis on lactate removal by the perfused rat kidney. 1. The isolated perfused kidneys of fed rats in normal acid-base status showed a constant rate of lactate removal from the perfusate between 5 and 90 min of perfusion at a perfusate pH of 7-4-7-5.
|
7e138e7d-198d-4862-8d76-93e0fe251c93
| 1 |
2. Lactate removal by kidneys of rats in normal acid-base status was stimulated within 30 min by a reduction in perfusate pH to 7-1-7-2, but depressed when perfusate pH was reduced further. 3. Kidneys taken from rats previously made acidotic and perfused with media of various pH values showed a progressive fall in the rate of lactate removal during the perfusion.
|
7e138e7d-198d-4862-8d76-93e0fe251c93
| 2 |
4. Glucose output by the kidneys of rats in normal acid-base status perfused with lactate as substrate was not affected by an alteration in perfusate pH. The kidneys of acidotic rats generally showed an increased rate of glucose output compared with those of control rats.
|
4267b23e-d8ca-4e2f-98dc-5ed109ade43c
| 0 |
Elastin--proteoglycan interaction. Conformational changes of alpha-elastin induced by the interaction. The interaction between alpha-elastin and a connective tissue proteoglycan was followed by optical density measurements and circular dichroism spectroscopy. It was found that interaction takes place at pH values below the isoelectric point of elastin with the formation of a complex coacervate. CD spectra demonstrated conformational changes of alpha-elastin caused by the interaction and resulting in an increase in the content of helical structure. This finding suggests the possibility of the involvement of proteoglycans in the molecular organization of elastin.
|
3858e70f-b5f2-4446-ab03-3aa5a02dc864
| 0 |
Bilateral cryptorchidism in a bull. Clinical and pathological observations were made on a case of bilateral cryptorchidism in a bull. Sexual libido could not be assessed because the bull was housed alone. The location of the intraabdominal testes indicated that surgical castration would necessitate a flank laparotomy incision.
|
9c8dd1b6-3f5f-4f8d-acfc-9d6cf0393029
| 0 |
Treatment of tardive dyskinesia. The pathogenesis of tardive dyskinesia is distinct from and may be functionally opposite to that of parkinsonism. The former is thought to be related to central nervous system dopaminergic hyperactivity, while the latter is known to be related to dopamine deficiency. An effective schema for the treatment of tardive dyskinesia includes avoiding antiparkinsonian medication and prescribing deanol, an acetylcholine precursor, while continuing or increasing phenothiazine dosages.
|
5d96a2fe-e951-45fd-a321-927a6004e391
| 0 |
Epidemiology of tardive dyskinesia Part I. We have performed an epidemiological study concerning tardive dyskinesia on a sample of 332 chronic schizophrenic patients (142 males and 190 females, mean age 48.6 years, mean duration of neuroleptic treatment 14.5 years). We could conclude that the age of patients at the time of assessment procedures is the most important variable.
|
5d96a2fe-e951-45fd-a321-927a6004e391
| 1 |
The prevalence of tardive dyskinesia was significantly higher in the older population. The significance of an insidious beginning of the illness might be only secondary to the highly significant role of the age. Other factors, such as sex, type of schizophrenia, initial syndrome, present psychic state, organic syndromes and neuroleptic-induced extrapyramidal syndrome, do not seen to play a role in the prevalence of tardive dyskinesia.
|
dd9f30e8-4d16-4001-965f-5f2a83329764
| 0 |
Postnatal development of the circadian rhythm of rat liver tyrosine aminotransferase activity. The rhythm of tyrosine aminotransferase (TAT) activity in 2-day old rats is characterized by a maximum at the beginning and a further one at the end of light-time. In 7-day old animals, the rhythm is much less pronounced than in 2-day old pups.
|
dd9f30e8-4d16-4001-965f-5f2a83329764
| 1 |
At the 21st day of life, the rats already exhibit the rhythmic pattern of the adults, although the absolute values are still somewhat below those of the adults. The TAT rhythm in neonates is obviously generated by periodic variations in cyclic AMP-dependent release of TAT from polysomes.
|
bdf66c74-61b6-4c1a-b756-29e9b9da6f6a
| 0 |
The influence of dehydrocholate on hepatic uptake and biliary excretion of 3H-taurocholate and 3H-ouabain. The hepatic uptake and biliary excretion of 3H-taurocholate and 3H-ouabain was studied in the rat during saline (control) and dehydrocholate infusions. Dehydrocholate (140 mumol/hr) did not influence the plasma disappearance nor the biliary excretion of taurocholate after a single iv injection (37 mumol/kg).
|
bdf66c74-61b6-4c1a-b756-29e9b9da6f6a
| 1 |
Bile production in the dehydrocholate experiment was increased 2- to 3-fold compared with controls. The biliary transport maximum for exogenously administered taurocholate was determined by constant infusion to be 135.0 +/- 3.0 mumol/hr (22 mumol/min/g of liver). Concomitant infusions of 140 mumol of dehydrocholate per hr did not alter the maximal taurocholate output.
|
bdf66c74-61b6-4c1a-b756-29e9b9da6f6a
| 2 |
The effects of the two bile salts on bile flow were additive. Dehydrocholate (140 mumol/hr) reduced the biliary excretion of 3H-ouabain (0.8 mumol/kg) and elevated the secondary slow component of the plasma disappearance of the cardiac glycoside. The hepatic levels of ouabain were increased compared with controls.
|
bdf66c74-61b6-4c1a-b756-29e9b9da6f6a
| 3 |
It is concluded that dehydrocholate interferes with ouabain transport at the canalicular level but not with primary hepatic uptake. Taurocholate (140 mumol/hr) failed to influence the total biliary output of ouabain. These differences and the lack of interaction between dehydrocholate and taurocholate suggest a hepatic transporting pathway for taurocholate which differs from that for taurocholate which differs from that for dehydrocholate and/or its metabolites.
|
5fceab96-31ca-418f-802c-48de9b36d7ab
| 0 |
Postnatal development of mixed-function oxidation as measured in microsomes from the small intestine and liver of rabbits. The postnatal development of aminopyrine N-demethylase, aniline 4-hydroxylase, benzpyrene hydroxylase, biphenyl 4-hydroxylase, 7-ethoxycoumarin 0-deethylase activities, NADPH-cytochrome c reductase, and cytochrome P-450 was compared in microsomes from the liver and small intestine of New Zealand white rabbits.
|
5fceab96-31ca-418f-802c-48de9b36d7ab
| 1 |
Apart from hepatic aniline hydroxylase activity, all of the xenobiotic-metabolizing enzyme activities examined had a similar pattern of development in the liver and small intestine. In both tissues the ability to metabolize xenobiotics was generally undetectable at 2 days of age and remained relatively low for the first 20 days of life.
|
5fceab96-31ca-418f-802c-48de9b36d7ab
| 2 |
Theresfter, a rapid 2- to 5-fold increase in all the enzyme activity studied was noted, and adult values were reached or exceeded by 30 days of age. Subsequent development of xenobiotic-metabolizing enzyme activities in the small intestine, but not in the liver, exhibited a transient fall at 50 days of age before adult activities were attained after 75 days of age.
|
5fceab96-31ca-418f-802c-48de9b36d7ab
| 3 |
The developmental pattern of cytochrome P-450 in the small intestine closely resembled that of the xenobiotic-metabolizing enzyme activities, but in the liver this correlation was less exact.
|
c00df33f-b275-40d6-a340-e23bee745fbd
| 0 |
Characterization of the hepatic microsomal mixed-function oxidase enzyme system in miniature pigs. Hepatic microsomal protein, cytochrome P-450, UDP-glucuronyltransferase, ethylmorphine demethylase, aniline hydroxylase, and aryl hydrocarbon hydroxylase levels were measured in the 2-, 4-, 5-, 6-, and 8-month-old Hanford miniature pig. The activities or concentrations of all of the liver parameters measured had apparently reached their adult plateau level by 2 months of age. The use of the miniature pig in toxicology research programs is discussed.
|
724aae56-9006-4463-a63e-9a387265bd12
| 0 |
Monooxygenase-catalyzed aldrin epoxidation and dihydroisodrin hydroxylation in monkey liver needle-biopsy specimens. Assay and properties. Aldrin epoxidation and dihydroisodrin (1,8,9,10,11,11-hexachloro-2,3-7,6-endo-2,1-7,8-endo-tetracyclo [6.2.1.1(3), (6).0(2), (7)]dodec-9-ene (DHI) hydroxylation have been studied in 0.2
|
724aae56-9006-4463-a63e-9a387265bd12
| 1 |
-ml liver monooxygenase preparations. Liver biopsy specimens of rhesus (Macaca mulatta) and bonnet (M. radiata) monkeys obtained with a 1.9-mm Menghini needle were the primary enzyme sources. Dieldrin and monohydroxydihydroisodrin (DHI-OH) were the only metabolites detected by electron-capture GLC analysis of hexane extracts of incubation media.
|
724aae56-9006-4463-a63e-9a387265bd12
| 2 |
Incubation, extraction, and analysis could be done in the same vessel. Maximum rates were obtained in the presence of NADPH and O2, and both transformations were inhibited by CO. The apparent KM and Vmax (+/-SD) for epoxidation was 1.2 +/- 0.2 X 10(-5) M aldrin and 210 +/- 20 pmol of dieldrin per mg of protein per min, and the corresponding values for hydroxylation were 2.3
|
724aae56-9006-4463-a63e-9a387265bd12
| 3 |
+/- 0.4 X 10(-5) M DHI and 150 +/- 20 pmol of DHI-OH per mg of protein per min. Aldrin epoxidation and DHI hydroxylation activities of rhesus monkey liver biopsy and rat liver preparations were evaluated after phenobarbital treatment. The assay procedures can be used in protocols in which animals serve as their own controls.
|
7ad2f19d-ae05-47e5-af00-fafca965596d
| 0 |
In vitro metabolism of 1-phenyl-2-propanone oxime in rat liver homogenates. 1-Phenyl-2-propanone oxime is a known in vitro metabolite of amphetamine. Further in vitro metabolism of this oxime with the 12,000g supernatant fraction from homogenized rat liver gave one major and two minor metabolites which were identified as 2-nitro-1-phenylpropane, benzyl alcohol, and 1-phenyl-2-propanone, respectively, by means of combined gas chromatography and mass spectrometry, and by comparison with authentic samples of each product.
|
5eaaec49-b72d-4385-b6a3-ba39b6f492e1
| 0 |
Anaerobic release of fluoride from halothane. Relationship to the binding of halothane metabolites to hepatic cellular constituents. Halothane has been found to undergo a reductive defluorination. This reaction requires an active cytochrome P-450 system and NADPH, and is inducible by phenobarbital and polychlorinated biphenyls but not by methylcholanthrene.
|
5eaaec49-b72d-4385-b6a3-ba39b6f492e1
| 1 |
The fluoride release occurs only under low O2 tension, while high O2 tension results in the oxidation of halothane to trifluoroacetic acid, inorganic bromide, and chloride. The release of the inorganic fluoride is linear up to 60 min. Because the conditions required for fluoride release and the binding of a halothane metabolite to microsomal phospholipids are similar, the defluorinated halothane molecule is assumed to be involved with this binding.
|
5eaaec49-b72d-4385-b6a3-ba39b6f492e1
| 2 |
However, based on the amount of fluoride released, the defluorinated halothane metabolite represents only approximately 60% of the total amount of halothane metabolite bound, which suggests that more than one metabolite may be involved in the binding.
|
580876ef-904c-4689-8224-33ecba1dfc2c
| 0 |
Microsomal spectral properties and narcotic N-demethylase activity in methadone-dependent rats. Rats were given access ad lib. to various concentrations (0.3 to 1.0 mg/ml) of methadone hydrochloride dissolved in sucrose solution. The N-demethylation of various narcotics was studied in hepatic preparations from methadone-consuming rats in order to determine if there was substrate specificity for the microsomal demethylase system.
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580876ef-904c-4689-8224-33ecba1dfc2c
| 1 |
The Vmax for the N-demethylation of methadone, ethylmorphine, and meperidine was increased by 40-65%, whereas that for morphine N-demethylation was reduced to 55% of the control value. Additive or synergistic effects on microsomal cytochrome P-450 content were seen when methadone consumption was supplemented by administration of maximally inducing doses of either 3-methylcholanthrene (3-MC) or phenobarbital (PB).
|
580876ef-904c-4689-8224-33ecba1dfc2c
| 2 |
This suggested that there was an increase in a type of cytochrome P-450 which was independent of that induced by PB or 3-MC. The qualitative change in cytochrome P-450 reflected in the ethylisocyanide binding spectrum was also apparent after treatment with methadone, PB, or 3-MC, and the combination of methadone and PB exhibited effects that differed from PB alone.
|
580876ef-904c-4689-8224-33ecba1dfc2c
| 3 |
Two-substrate kinetic analysis with methadone and morphine as substrates indicated that more than one enzymic system may be involved in the N-demethylation reaction and that a common component of this N-demethylase system could not be induced with phenobarbital. However, methadone and meperidine seem to be demethylated by the same enzymic system.
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68ed335b-e28d-4545-a685-3a24988a4f1d
| 0 |
Metabolism of 2-(3-chloro-4(4-chlorobenzoyl)-phenyl)-as-triazine-3,5(2H,4H)-dione by the chicken. The metabolism of the anticoccidial 2-[3-chloro-4-(4-chlorobenzoyl)phenyl]-as-triazine-3,-5(2H,4H)-dione (CP-25,415) was investigated in the chicken.
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68ed335b-e28d-4545-a685-3a24988a4f1d
| 1 |
It was shown that the predominant residue present in the chicken was 2-[3-chloro-4-(alpha-hydroxy-4-chlorobenzoyl)phenyl]-as-triazine-3,5(2H,4H)-dione (CP-25,641). A gas-liquid chromatographic assay for the analysis of CP-25,641 in biological fluids and tissues was developed which was rapid, accurate, and reproducible.
|
68ed335b-e28d-4545-a685-3a24988a4f1d
| 2 |
Results of the analytical method correlated well with radiochemical measurements and were indicative of the total drug-related residues. The half-life of CP-25,641 in tissues was approximately 32 hr except in the kidney, where the half-life was approximately 40 hr due to urine retention by the kidneys.
|
68ed335b-e28d-4545-a685-3a24988a4f1d
| 3 |
CP-25,641 was excreted without further change.
|
e39641ef-a213-436a-ba9b-f9512aeb8dba
| 0 |
Physiological disposition and metabolism of N-t-butylarterenol and its di-p-toluate ester (bitolterol) in the rat. The metabolism and disposition of the bronchodilator, N-t-butylarterenol (tBA) and its di-p-toluate ester (bitolterol) were compared in the rat. Radioactivity was preferentially retained in lungs of rats compared with heart and blood after iv medication with tritium-labeled bitolterol, but was not retained in tissues after iv medication with [3H]tBA.
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e39641ef-a213-436a-ba9b-f9512aeb8dba
| 1 |
After oral and iv medication with [3H]bitolterol, fecal radioactivity accounted for 24% of the dose and 65 and 79% of the radioactivity, respectively, was excreted in urine (0-72 hr). In comparison, urine radioactivity after oral and iv medication with [3H]tBA was 43 and 83% of the dose, respectively, and fecal radioactivity accounted for 43 or 23% of the dose, respectively (0-72 hr).
|
e39641ef-a213-436a-ba9b-f9512aeb8dba
| 2 |
Bitolterol was hydrolyzed in vitro to tBA by esterases found in various tissues including small intestine, liver, and plasma. Moreover, tBA was a substrate for catecholamine O-methyltransferase but not for monoamine oxidase. Similar metabolites were observed in urine samples of rats given either [3H]tBA or [3H]bitolterol.
|
e39641ef-a213-436a-ba9b-f9512aeb8dba
| 3 |
Urine metabolites were identified as free and conjugated forms of both tBA and 3-O-methyl-tBA.
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eb335f71-dd7f-469c-a39b-8edd172e83e9
| 0 |
Physiological disposition and metabolism of (3H)bitolterol in man and dog. The metabolism and disposition of bitolterol, the di-p-toluate ester of N-t-butylarterenol (tBA) was studied in man after a single oral dose and in dog after intraduodenal, iv, or oral administration.
|
eb335f71-dd7f-469c-a39b-8edd172e83e9
| 1 |
The mean (+/- SE) peak plasma radioactivity in man (dose, 70 mug/kg) was 180 +/- 18 ng equivalents of [3H]bitolterol per ml or approximately 11% of the dose, whereas peak plasma radioactivity in dog (dose, 200 mug/kg) was 144 +/- 23 ng equivalents per ml or approximately 4% of the dose. For both man and dog, the time for maximum plasma level of radioactivity varied from 0.5
|
eb335f71-dd7f-469c-a39b-8edd172e83e9
| 2 |
to 2 hr. In man, only 1% of the plasma radioactivity represented intact [3H]bitolterol 1.0 hr after medication. In the dog, radioactivity was concentrated in lung tissue after iv administration of [3H]bitolterol. Recovery of intact [3H]bitolterol in lung at 4.5 hr ranged from 26 to 46% of total tissue radioactivity after iv dosage and from 4 to 14% total tissue radioactivity after intraduodenal administration.
|
eb335f71-dd7f-469c-a39b-8edd172e83e9
| 3 |
Radioactivity recovered in human urine and feces (0-72 hr) accounted for 86 and 8.1% of the dose, respectively. Recovery of radioactivity in dog urine and feces accounted for 58 and 23% of the dose, respectively, in the same time period. Radiochromatograms of urine samples from man and dog revealed similar patterns of metabolites including free and conjugated forms of both tBA and the 3-O-methyl metabolite, N-t-butylmetarterenol.
|
eb335f71-dd7f-469c-a39b-8edd172e83e9
| 4 |
The major radioactive components of the feces were bitolterol and tBA. The results indicate that bitolterol is absorbed orally and retained as the intact ester in lung. The prolonged bronchodilator activity of bitolterol is due to the slow release of the ester from lung and hydrolysis to tBA, an active beta2-adrenoceptor agonist.
|
eb335f71-dd7f-469c-a39b-8edd172e83e9
| 5 |
Pharmacological activity is terminated by metabolism of tBA via conjugation or 3-O-methylation.
|
ce1cbcd4-2b4b-4098-96f7-ac1f4cb7f864
| 0 |
Adriamycin metabolism in man. Evidence from urinary metabolites. We studied the human metabolism of adriamycin by isolating and identifying urinary metabolites which retain adriamycin's specific fluorescence properties. Metabolites were extracted by adsorption to polystyrene polymeric sorbants, separated on silicic acid columns and purified by thin-layer chromatography.
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ce1cbcd4-2b4b-4098-96f7-ac1f4cb7f864
| 1 |
Structures were determined by comparative chromatography; infrared, fluorescence, and mass spectroscopy; and enzymatic and chemical degradation. Substances identified were adriamycinol, adriamycinol aglycone, adriamycin aglycone, deoxyadriamycin aglycone, deoxyadriamycinol aglycone, demethyldeoxyadriamycinol aglycone, demethyldeoxyadriamycinol aglycone 4-O-sulfate, and demethyldeoxyadriamycinol aglycone 4-O-beta-glucuronide. Other metabolites have been purified but not identified.
|
ce1cbcd4-2b4b-4098-96f7-ac1f4cb7f864
| 2 |
Human metabolism of adriamycin involved carbonyl reduction, reductive glycosidic cleavage, hydrolytic glycosidic cleavage, O-demethylation, O-sulfation, and O-beta-glucuronidation. Carbonyl reduction was the major enzymatic conversion occurring in the human.
|
bcf83eeb-4344-4a67-99ca-e198ce785d57
| 0 |
[Termination of pregnancy and perinatal mortality (author's transl)]. Elective induction was practised in 1875 of 10 537 deliveries (17.8%). Duration of delivery was, if anything, shortened after elective induction, compared with spontaneous delivery. There was no evidence of soft-tissue dystocias after elective induction.
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bcf83eeb-4344-4a67-99ca-e198ce785d57
| 1 |
The Apgar score was 8-10 in 95.7% of children born after elective induction. pH of umbilical-artery blood in 95.7% of children after elective induction was greater than or equal to 7.2. There was a striking increase in the incidence of occiput posterior position with elective induction (2.7
|
bcf83eeb-4344-4a67-99ca-e198ce785d57
| 2 |
% of cases). The incidence of operative vaginal delivery was as frequent after elective as after all other forms of delivery. The incidence of section was 4.7% after elective induction, 11.5% in the entire series, intra-uterine asphyxia being an indication in 1.7%, compared with 2.5
|
bcf83eeb-4344-4a67-99ca-e198ce785d57
| 3 |
% for the total group. The frequency of operations was inversely proportional to the cervical index. Perinatal mortality was 0.53 per thousand (one case) after elective induction, 10.15 per thousand in the total group, 5.9 per thousand in those with indication for early induction. Perinatal mortality decreased from 23.0
|
bcf83eeb-4344-4a67-99ca-e198ce785d57
| 4 |
per thousand to 7.2 per thousand from 1967 to 1974.
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b122036a-0866-4793-8cd7-200b2593ae63
| 0 |
Binding of organic compounds to rat liver and lung. The binding of various radioisotopically labeled organic compounds to rat liver and lung was investigated in vitro. Pieces of rat lung and slices of rat liver were incubated at 37 degrees C under a nitrogen atmosphere in a modified Krebs-Ringer phosphate solution (pH 7.4
|
b122036a-0866-4793-8cd7-200b2593ae63
| 1 |
) CONTAININg the compound to be studied. Of the neutral compounds investigated, digitoxin, digoxin and dexamethasone were highly bound to both liver and lung tissue, whereas the degree of binding of amitrole, erythritol, and ouabain was 20% or less. The weak acids which were bound to the greatest extent in both liver and lung were phenobarbital, pentobarbital, and diphenylhydantoin.
|
b122036a-0866-4793-8cd7-200b2593ae63
| 2 |
Barbital was poorly bound, and there was no evidence for the binding of 5,5-dimethyloxazolidine-2,4-dione or p-aminohippuric acid in either tissue. Binding of the cardiac glycosides and the barbiturates directly paralleled their lipid solubilities. The degree of binding of neutral compounds and weak acids to lung and liver tissue did not vary greatly with concentration, even though broad concentration ranges were studied.
|
b122036a-0866-4793-8cd7-200b2593ae63
| 3 |
This was also true of the weak base morphine. On the other hand, the binding to liver and lung of the organic bases nicotine, pilocarpine, d-amphetamine, lidocaine, erythromycin, and chloroquine, did vary with concentration. The quaternary ammonium compound decamethonium was bound only to liver, and this binding also varied with concentration.
|
b122036a-0866-4793-8cd7-200b2593ae63
| 4 |
Two additional quaternary ammonium compounds, tetraethylammonium and N1-methylnicotinamide, were not significantly bound to either tissue. Comparisons on the basis of equal content of solids revealed that the binding of diverse organic compounds in liver is greater than or equal to that in lung.
|
461b54cb-8588-493b-914e-42cac626a7f7
| 0 |
Pharmacokinetics of digoxin in the rat. Previous studies on the pharmacokinetics of 3H-digoxin in the rat have been based on total radioactivity in the plasma, even though the drug is extensively metabolized in this species. A comparison of total radioactivity vs. unchanged drug in rat plasma after administration of 3H-digoxin clearly showed the need to separate digoxin from its metabolites.
|
461b54cb-8588-493b-914e-42cac626a7f7
| 1 |
The pharmacokinetics of digoxin were therefore examined using solvent extraction and thin-layer chromatography to isolate unchanged drug. Digoxin levels after a 1 mg/kg iv dose were measured in the plasma and urine of adult male rats in which the bile duct or the ureters had been ligated, as well as in sham-operated controls.
|
461b54cb-8588-493b-914e-42cac626a7f7
| 2 |
In all cases, digoxin concentrations were best described by a two-compartment open model. Digoxin was rapidly eliminated from the plasma of controls, with a half-life of 2.5 hr, a volume of distribution of 3.6 liter/kg, and a renal clearance somewhat lower than the glomerular filtration rate.
|
461b54cb-8588-493b-914e-42cac626a7f7
| 3 |
No significant change in these parameters was observed in rats with bile duct ligation. The total body clearance of 5.77 ml/min in the controls was reduced by only 10% in the bile duct-ligated rats. In animals with bilateral ureter ligation, the body clearance was reduced by 30% and the plasma half-life of digoxin was increased to 4 hr, although no significant change in the apparent volume of distribution was noted.
|
461b54cb-8588-493b-914e-42cac626a7f7
| 4 |
Approximately 60% of the total body clearance was unaffected by bile duct and ureter ligations, and was assumed to be due to biotransformation. Biliary excretion was found to be important for digoxigenin bisdigitoxoside, inasmuch as rats with bile duct ligation showed elevated metabolite levels in the plasma as well as a 3-fold increase in renal excretion of the bisglycoside.
|
9d948635-8fc4-4322-8732-6e015abddabe
| 0 |
N-acetylation of drugs. Pharmacogenetic studies in rabbits selected for their acetylator characteristics. Studies on acetylation of sulfadiazine, isoniazid, and p-aminobenzoic acid in selected lines of slow and rapid acetylator rabbits are described. Pedigree analysis of rabbits classified as slow or rapid sulfadiazine acetylators confirmed previous studies that the rate of sulfadiazine elimination (acetylation) is genetically controlled, with rapid elimination dominant over slow elimination of the drug.
|
9d948635-8fc4-4322-8732-6e015abddabe
| 1 |
Pharmacokinetic studies in rabbits of specified sulfadiazine acetylator genotypes with isoniazid and p-aminobenzoic acid show that the rate of isoniazid elimination is under the same genetic control as is sulfadiazine, whereas the rate of p-aminobenzoic acid elimination is not. A new drug acetylation polymorphism, which controls the rate of enzymatic acetylation of p-aminobenzoic acid in peripheral blood cells and which is related to the sulfadiazine acetylation polymorphism, is described.
|
247f7c2c-814d-42cc-9a4c-a14863a85dec
| 0 |
Histidyl transfer ribonucleic acid synthetase from Salmonella typhimurium. Interaction with substrates and ATP analogues. Structural requirements for substrate binding to histidyl-tRNA synthetase from Salmonella typhimurium have been investigated using ATP analogues. Ki values and the relative binding affinity of the enzyme for these analogues have been determined in the tRNA aminoacylation reaction.
|
247f7c2c-814d-42cc-9a4c-a14863a85dec
| 1 |
The enzyme is highly specific for ATP: no binding was found for GTP, CTP, TTP and UTP. dATP is a very poor substrate for acylation of tRNA, with a Km 40-fold higher than that of ATP. Binding of adenosine 5'-triphosphate requires interactions of the amino group of adenosine and the sugar moiety;
|
247f7c2c-814d-42cc-9a4c-a14863a85dec
| 2 |
the 2' and the 5' positions of the ribose appear to be essential for recognition; the phosphate groups enhance the binding. AMP is a noncompetitive inhibitor with ATP. The interaction of histidyl-tRNA synthetase, a dimeric enzyme, with histidine and ATP was examined by fluorescence measurements at equilibrium and by equilibrium dialysis.
|
247f7c2c-814d-42cc-9a4c-a14863a85dec
| 3 |
Binding with L-histidine is significantly tighter at pH 6 than at pH 7, while the ATP binding is independent of pH. The stoichiometry was measured at pH 6 than at pH 7, while the ATP binding is independent of pH. The stoichiometry was measured at pH 7.5
|
247f7c2c-814d-42cc-9a4c-a14863a85dec
| 4 |
by equilibrium dialysis and is 1 mol ATP/mol enzyme and, variably, close to 2 or 1 mol histidine/mol enzyme.
|
25d0c657-46bf-42db-9b69-6603bae1b702
| 0 |
[The coupling of beta1-24-corticotropin to the adenylate-cylase system in rat adipocytes. Evidence for hormone-nucleotides interaction (author's transl)]. The general aim was to define some of the most important parameters involved in the coupling step between the synthetic analog of adrenocoricotropin hormone (beta1-24-corticotropin tetracosa peptide) and the catalytic unit of the adenylate-cyclase system of fat cells.
|
25d0c657-46bf-42db-9b69-6603bae1b702
| 1 |
These studies were performed with a purified plasma membrane fraction from rat adipose tissue. In this regard, some effects of ions, pH, and nucleotides (ATP nad GTP) on this hormone sensitive system were studied A simple model based on a random association process of reactants yeilded a statisfactory approximation of the kinetic data.
|
25d0c657-46bf-42db-9b69-6603bae1b702
| 2 |
In contract to results obtained by two other groups, which were analyzed by De Haen, no evidence was found for a regulation of the adenylate-cyclase activity by the adenosine triphosphate which was not complexed to magnesium...
|
c13c49d4-6c4a-4a22-a4a7-9b60528a2e2f
| 0 |
Ion-binding to phospholipids. Interaction of calcium with phosphatidylserine. The binding of Ca2+ to monolayers and bilayers of phosphatidylserine has been investigated as a function of pH, ionic strength (NaCl concentration) and Ca2+ concentration using surface and colloid chemical techniques. The molar ratio of lipid to bound calcium decreases to 2 as the Ca2+ concentration is increased to about 0.1
|
c13c49d4-6c4a-4a22-a4a7-9b60528a2e2f
| 1 |
mM. At [Ca2+] greater than 0.1 mM a 1:1 complex is formed. The apparent binding constant Ka ranges from about approximately 10(6) - 10(4) l/mol depending on the Ca2+ concentration. After allowing for electrostatic effects and neighbour group interactions, the intrinsic binding constant Ki of the phosphorylserine polar group at pH 7 (I = 0.01
|
c13c49d4-6c4a-4a22-a4a7-9b60528a2e2f
| 2 |
M), where it carries a net negative charge of one, is approximately 10(4) l/mol; consistent values for Ki were obtained using several independent approaches. Ka for Ca2+ binding decreases with increasing NaCl concentration because the monovalent cations compete with Ca2+ for the same binding site.
|
c13c49d4-6c4a-4a22-a4a7-9b60528a2e2f
| 3 |
Na+ and K+ are equally effective in displacing 45Ca2+ adsorbed to monolayers of phosphatidylserine, both with respect to the kinetics and the equilibrium of the displacement. Ka for the reaction between phosphatidylserine and monovalent cations is about 10(3)-fold smaller than that of Ca2+. An investigation of the binding of Mn2+ to phosphatidylserine by both surface chemical and nuclear magnetic resonance methods shows that this cation has a similar binding constant to that of Ca2+.
|
c13c49d4-6c4a-4a22-a4a7-9b60528a2e2f
| 4 |
The Ca2+-binding capabilities of monolayers containing only carboxyl groups (i.e. arachidic acid) and phosphodiester groups (i.e. dicetyl phosphate) have also been determined; the apparent pK for the - COOH group in monolayers is larger than or equal to 9 and that for the phosphodiester group is less than 4.
|
c13c49d4-6c4a-4a22-a4a7-9b60528a2e2f
| 5 |
Since these groups do not retain the same pK values when they are in close proximity in the phosphorylserine group, the relative contributions of the two groups to the binding of Ca2+ to phosphatidylserine is not obvious.
|
2b53fb29-cd30-4524-a39e-1a78b2a6b146
| 0 |
Action of H1 and H2 inhibitors on the response of histamine sensitive adenyly cyclase from guinea-pig mucosa. In the guinea-pig, it has been shown that homogenates of mucosa from the fundus contain an adenylyl cyclase system that is activated by histamine as well as by prostaglandins PGE1 and PGA1.
|
2b53fb29-cd30-4524-a39e-1a78b2a6b146
| 1 |
The effects of burimamide, an H2-inhibitor, and mepyramine and chlorpheniramide, both H1-inhibitors, were tested. Both H1 and H2 inhibitors behaved kinetically as competitive inhibitors of histamine, but the Km derived for burimamide (2.5 - 4.1 . 10(-5)) was significantly lower than that for either chlorpheniramine (0.9
|
2b53fb29-cd30-4524-a39e-1a78b2a6b146
| 2 |
- 1.9 . 10(-4)) or mepyramine (1.3 - 1.4 . 10(-4)). On the other hand none of the three inhibitors influenced the cyclase activation by PGE1 and PGA1. These results suggest that there are at least two types of receptors in the preparation studied, one responsive to histamine and the other to the prostaglandins, and that the specificity of H1- and H2-receptors is not absolute in the broken cell preparation.
|
da316685-e8dc-4438-8912-124d86e46e9f
| 0 |
Anti-arrhythmic action of nadolol, a beta-adrenergic receptor blocking agent. The anti-arrhythmic action of 2,3-cis-1,2,3,4-tetrahydro-5-[(2-hydroxy-3-tert-butylamino)propoxy]2,3-naphthalenediol (nadolol) was evaluated and compared with that of propranolol in several experimental models of cardiac arrhythmias.
|
da316685-e8dc-4438-8912-124d86e46e9f
| 1 |
Both nadolol and propranolol antagonized isoproterenol-induced tachycardia and ouabain-induced arrhythmias in cats, antagonized coronary artery ligation-induced ventricular fibrillation and suppressed ventricular ectopic activity during vagal stimulation in dogs. In contrast to propranolol, nadolol was considerably weaker in suppressing existing digoxin-induced arrhythmias, lacked local anesthetic activity and did not depress the heart in dogs.
|
da316685-e8dc-4438-8912-124d86e46e9f
| 2 |
Because of these findings, it is concluded that the anti-arrhythmic activity of nadolol is apparently related to blockade of beta-adrenergic receptors.
|
f0487c0b-5afd-4c25-add5-cae4a22bedfa
| 0 |
Effects of chemical stimulation of the mesolimbic dopamine system upon locomotor activity. The effects of local injections of drugs into terminal areas of the mesolimbic dopamine system were investigated. Bilateral administration of dopamine, but not of noradrenaline and serotonin, into the nucleus accumbens of non-pretreated rats resulted in stimulation of locomotor activity.
|
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