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

被引:5
作者
FENG, PCC
SOLSTEN, RT
机构
[1] The Agricultural Group, Monsanto Co., St Louis, MO
关键词
D O I
10.3109/00498259409043273
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. Thiazopyr was metabolized by liver microsomes from male Sprague-Dawley rats to a previously unidentified metabolite. 2. The new metabolite was identified by coelution with an authentic standard in hplc and by electrospray lc/ms as the corresponding carboxylic acid. 3. Formation of the carboxylic acid metabolite was inhibited in the presence of mono-oxygenase inhibitors including piperonyl butoxide, 1-aminobenzotriazole, metyrapone and tetcyclacis. 4. Transformation of thiazopyr to its carboxylic acid by rat liver microsomes is mediated by mono-oxygenases and not hydrolases.
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页码:729 / 734
页数:6
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