Metabolism of diltiazem. III. Oxidative deamination of diltiazem in rat liver microsomes.
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چکیده
منابع مشابه
Short Communication Extensive Metabolism of Diltiazem and P-Glycoprotein-Mediated Efflux of Desacetyl- Diltiazem (M1) by Rat Jejunum In Vitro
The objective of this in vitro study was to investigate both the intestinal metabolism and transport of diltiazem (DTZ) and its major metabolites in rat jejunum. Metabolism experiments were performed with everted sacs, whereas sheets mounted in a symmetrical twin chamber system were used in transport studies. DTZ was rapidly desacetylated by the rat jejunum to the principle metabolite desacetyl...
متن کاملExtensive metabolism of diltiazem and P-glycoprotein-mediated efflux of desacetyl-diltiazem (M1) by rat jejunum in vitro.
The objective of this in vitro study was to investigate both the intestinal metabolism and transport of diltiazem (DTZ) and its major metabolites in rat jejunum. Metabolism experiments were performed with everted sacs, whereas sheets mounted in a symmetrical twin chamber system were used in transport studies. DTZ was rapidly desacetylated by the rat jejunum to the principle metabolite desacetyl...
متن کاملCharacterization of Species Differences in Tissue Diltiazem Deacetylation Identifies Ces2a as a Rat-Specific Diltiazem Deacetylase.
Diltiazem, a calcium channel blocker, is mainly metabolized via demethylation or deacetylation in humans. Diltiazem demethylation is catalyzed by cytochrome P450 2D6 and 3A4. Although it was previously reported that the area under the curve ratio of deacetyldiltiazem to diltiazem after oral dosing with diltiazem in rats was sevenfold higher than in humans, the molecular mechanisms underlying th...
متن کاملDigitoxin metabolism by rat liver microsomes.
published by admin on Fri, 03/14/2014 8:53am Title Digitoxin metabolism by rat liver microsomes. Publication Type Journal Article Year of Publication 1975 Authors Schmoldt, A, Benthe, HF, Haberland, G Journal Biochem Pharmacol Volume 24 Issue 17 Pagination 1639-41 Date Published 1975 Sep 1 ISSN 0006-2952
متن کاملPredicting drug interaction of diltiazem on microbial metabolism of midazolam
The present investigation was aimed at studying the biotransformation of midazolam, a marker substrate for CYP3A4 metabolic reactions using nine microbial cultures. The study was performed using a two stage fermentation protocol and the results indicate that the microbial cultures produce hydroxylated metabolites of midazolam, based on HPLC-DAD and LC-MS-MS analysis. The metabolism of midazolam...
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ژورنال
عنوان ژورنال: Journal of Pharmacobio-Dynamics
سال: 1990
ISSN: 0386-846X,1881-1353
DOI: 10.1248/bpb1978.13.612