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STEREOSELECTIVE DISPOSITION OF NAPROXEN GLUCURONIDE IN THE RAT

by Naproxen Glucuronide, Send Dr, Leslie Z. Benet, Department Of Pharmacy, Masahiro Iwaki, Alfred Bischer, Ann C. Nguyen, Antony F. Mcdonagh, Leslie, Z. Benet , 1995
"... The disposition of R- and S-naproxen glucuronides were investi-gated after intravenous administration (-1.5 mg/kg) to normal male Sprague-Dawley rats and to rats pretreated with phenyl-methylsulfonylfluoride, an inhibitor of esterases. The relative sta-bility of the two glucuronides also was measure ..."
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The disposition of R- and S-naproxen glucuronides were investi-gated after intravenous administration (-1.5 mg/kg) to normal male Sprague-Dawley rats and to rats pretreated with phenyl-methylsulfonylfluoride, an inhibitor of esterases. The relative sta-bility of the two glucuronides also

METABOLIC DISPOSITION OF THE ACYCLOVIR PRODRUG VALACICLOVIR IN THE RAT

by Thimysta C Burnette , Paulo De Miranda
"... ABSTRACT: The to a final concentration of 10 mg/ml and 100 MCi/mi in sterile deionized water. At the specified times after dosing, the rats were decapitated (3/time point), and the following tissues were excised: brain, thymus, lung, heart, liver, mesenteric lymph nodes, stomach, small intestine (a ..."
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ABSTRACT: The to a final concentration of 10 mg/ml and 100 MCi/mi in sterile deionized water. At the specified times after dosing, the rats were decapitated (3/time point), and the following tissues were excised: brain, thymus, lung, heart, liver, mesenteric lymph nodes, stomach, small intestine

Drug Absorption-Disposition Model Corresponding author:

by Helen H. Usansky, Patrick J. Sinko, Patrick J. Sinko , 2005
"... Number of text pages: 18 Number of tables: 3 Number of figures: 4 Number of references: 54 Number of words in abstract: 248 Number of words in introduction: 841 Number of words in discussion: 1499 List of abbreviations: Fa, the fraction of drug taken up into intestinal tissue; Fgw, the fraction esca ..."
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, the first-order rate constants of gastric empting, intestinal transit, absorption and elimination from plasma, respectively; Pm, intestinal transcellular permeability; S, intestinal absorptive surface area; Ms, Mi and Mpl, the 3 JPET #76182 amounts of drug in the stomach, intestine and plasma, respectively

METABOLIC DISPOSITION OF THE COGNITION ACTIVATOR TACRINE IN RATS, DOGS, AND HUMANS Species Comparisons

by William F Pool , Michael D Reily , Susan M Bjorge , Thomas F Woolf
"... ABSTRACT: The metabolic fate of tacrine [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate (THA)] was examined in rats, dogs, and humans. After administration of single oral doses of [ 14 C]THA to rats, dogs, and humans, drug-derived material was well absorbed, with urinary excretion ..."
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Laboratories (Ann Arbor, MI) (14) and shown to have radiochemical and chemical purities of Ͼ99%. Unlabeled THA and 1-, 2-, and 4-OH-THA (all of chemical purity Ͼ99%) were prepared by methods previously described (15). 7-OH-THA and the N-hydroxylamine derivative of THA (N-hydroxyl-THA) were synthesized using

THE PHYSIOLOGICAL DISPOSITION 01 ” PROBENECID, INCLUDINC; RENAL CLEARANCE, IN MAN, STUDIEI) BY AN IMPROVED METHOD FOR ITS ESTIMATION IN BIOLOGICAL MATERIAL1’

by Peter G. L)ayton, T. F. Vt, W. Chen, Ia. Behgeh, L. A. West, A. B. Glitman , 1963
"... In the course of a study of the interactiotis of uricosuric agents in man (Yu ci a!., 1962), it became necessary to measure the renal clear-ance of probenecid (Ilenemid) (fig. 1). Such clearance nieasurcments have 1)een recorded in dogs (l3eyer, 1954; Weiner et a!., 1960) but the published methods ..."
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suitable for our purpose, and for investigation oof (other aspects of the physiological disposition of lorol)ene(i(l. METHODS. Thme presemit method involves the separat 1(011 (of prothenecid frooni acid fled! bi ol (ogical material by ext ract ion imit 0 et hivlene dichiloride, After separat ioomi, t lie

Printed in U.S.A. ORAL ABSORPTION AND DISPOSITION KINETICS OF LIDOCAINE HYDROCHLORIDE IN DOGS

by R. N. Boyes, H. J. Adams, B. R. Duce , 1970
"... levels of lidocaine hydrochloride in six beagles were determined after the administration of 31 mg/kg by: 1) a 1-hour constant rate i.v. infusion, 2) an exponential i.v. infusion having a half-time of 40 minutes and 3) p.o. administration in solution. A mean peak blood level of 9.2 pg/nil (range, 7. ..."
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.1-11.1) occurred 60 minutes after the constant rate i.v. infusion was started. The exponential i.v. infusion resulted in a mean peak blood level of 5.6 pg/ml (range, 4.7-7.5) 30 minutes after starting the infusion. After p.o. administration a mean peak blood level of 4.4 pg/mi (range, 3.1-6.8) occurred at 45

THE JOURNAL OF PHARMACOLOGY ANDEXPERIMENTAL THEaaPEurics Interaction of Verapamil andCimetidine: Stereochemical Aspects of DrugMetabolism, DrugDisposition andDrugAction'

by Gerd Mikus , Michel Eichelbaum , Christine Fischer , Stanislaw Gumulka , Ulrich Klotz , Heyo K Kroemer
"... ABSTRACT The pharmacokinetics, metabolism and pharmacodynamics of verapamil (160 mg p.o. of a pseudoracemic mixture) were eval uated in six healthy volunteers before and after coadministration of cimetidine (400 mg b.i.d.). Enantiomers of verapamil and enantiomers of three major urinary metabolites ..."
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metabolites (norverapamil, D 617 and 0-620) were determined in plasma and urine by gas chromatography-mass spectrometry. Coadministration of cime tidine led to a significant increase in the area under the plasma concentration vs. time curve of S-verapamil (29.2 ±31 .8 mm x nmol x mI-1 vs. 41.2 ±33.7 mm x

MicroRNA-328 negatively regulates the expression of breast cancer resistance protein (BCRP/ABCG2) in human cancer cells

by Yu-zhuo Pan, Marilyn E. Morris, Ai-ming Yu - Mol Pharmacol , 2009
"... Breast cancer resistance protein (BCRP/ABCG2) is a molecular determinant of pharmacokinetic properties of many drugs in humans. To understand post-transcriptional regulation of ABCG2 and the role of microRNAs (miRNAs) in drug disposi-tion, we found that microRNA-328 (miR-328) might readily tar-get t ..."
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Breast cancer resistance protein (BCRP/ABCG2) is a molecular determinant of pharmacokinetic properties of many drugs in humans. To understand post-transcriptional regulation of ABCG2 and the role of microRNAs (miRNAs) in drug disposi-tion, we found that microRNA-328 (miR-328) might readily tar

Additive effects of the chemokine receptor 2, vitamin D receptor, interleukin-6 polymorphisms and cardiovascular risk factors on the prevalence of myocardial infarction in patients below 65 years

by Jan R Ortlepp , Constanze Krantz , Melanie Kimmel , Alexei Von Korff , Katharina Vesper , Fabian Schmitz , Vera Mevissen , Uwe Janssens , Andreas Franke , Peter Hanrath , Klaus Zerres , Rainer Hoffmann
"... Abstract Background: Cardiovascular risk factors (CRF) have been associated with myocardial infarction (MI), while the role of genetic risk factors (GRF) remains undetermined. Methods: Cineventriculograms of 3436 were analyzed for presence of regional function impairment as sign of MI. Genotyping f ..."
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) the combination of CRF was only weakly associated with MI, while GRF were not. In these patients age was a predictor of MI. Conclusion: Certain GRF might have additive but small effects on the disposition for MI before the age of 65. In older patients the tested GRF had no effect, possibly indicating a mechanism

Are Differences in MicroRNA Regulation Implicated in Species- Dependent Response to Toxicological Exposures?

by Costas Koufaris, Nigel J. Gooderham , 2012
"... Equivalent exposures can result in qualitatively or quantita tively dissimilar toxic effects across species, with the underlying molecular mechanisms being often not well defined. In many cases, differences in metabolic handling of the chemical (metabo lism and disposition) provide an explanation of ..."
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Equivalent exposures can result in qualitatively or quantita tively dissimilar toxic effects across species, with the underlying molecular mechanisms being often not well defined. In many cases, differences in metabolic handling of the chemical (metabo lism and disposition) provide an explanation
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