IN-VITRO BIOTRANSFORMATION OF THIAZOPYR BY RAT-LIVER MICROSOMES - OXIDATIVE CLEAVAGE OF A CARBOXYLIC METHYLESTER BY MONOOXYGENASES

Authors
FENG PCC SOLSTEN RT
Citation
Pcc. Feng et Rt. Solsten, IN-VITRO BIOTRANSFORMATION OF THIAZOPYR BY RAT-LIVER MICROSOMES - OXIDATIVE CLEAVAGE OF A CARBOXYLIC METHYLESTER BY MONOOXYGENASES, Xenobiotica, 24(8), 1994, pp. 729-734
Citations number
12
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
Xenobiotica → ACNP
ISSN journal
00498254
Volume
24
Issue
8
Year of publication
1994
Pages
729 - 734
Database
ISI
SICI code
0049-8254(1994)24:8<729:IBOTBR>2.0.ZU;2-G
Abstract
1. Thiazopyr was metabolized by liver microsomes from male Sprague-Daw ley rats to a previously unidentified metabolite. 2. The new metabolit e was identified by coelution with an authentic standard in hplc and b y electrospray lc/ms as the corresponding carboxylic acid. 3. Formatio n of the carboxylic acid metabolite was inhibited in the presence of m ono-oxygenase inhibitors including piperonyl butoxide, 1-aminobenzotri azole, metyrapone and tetcyclacis. 4. Transformation of thiazopyr to i ts carboxylic acid by rat liver microsomes is mediated by mono-oxygena ses and not hydrolases.