Biliary metabolites of semotiadil fumarate in the rat

After oral administration of 14C-semotiadil fumarate to rat, 81.3% of the dosed radioactivity was excreted into the bile. Five major biliary metabolites were detected and characterized as phenolic O-glucuronides by FAB mass spectrometry and 1H-nmr spectrometry. From these results it was concluded th...

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Bibliographic Details
Published inXenobiotica Vol. 25; no. 8; p. 847
Main Authors Nakaoka, M, Katoh, K, Hakusui, H
Format Journal Article
LanguageEnglish
Published England 1995
Subjects
Animals
Bile - metabolism
Biotransformation
Calcium Channel Blockers - metabolism
Calcium Channel Blockers - pharmacokinetics
Chromatography, High Pressure Liquid
Glucuronates - chemistry
Glucuronates - metabolism
Magnetic Resonance Spectroscopy
Male
Molecular Structure
Oxidation-Reduction
Rats
Rats, Wistar
Spectrometry, Mass, Fast Atom Bombardment
Thiazoles - metabolism
Thiazoles - pharmacokinetics
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Summary:After oral administration of 14C-semotiadil fumarate to rat, 81.3% of the dosed radioactivity was excreted into the bile. Five major biliary metabolites were detected and characterized as phenolic O-glucuronides by FAB mass spectrometry and 1H-nmr spectrometry. From these results it was concluded that the first step in the metabolism of semotiadil in rat was oxidations at various portions around the molecule to produce phenols. These oxidations implied the ring-opening of the methylenedioxy ring, O-demethylation of the methoxybenzene, hydroxylation of the ring, and aromatic N-demethylation. The next step was O-glucuronidation of the resulting intermediate phenolic metabolites.
ISSN:0049-8254
DOI:10.3109/00498259509061898