The formation of thiobenzamide-S-oxide (TBSO) from thiobenzamide (TB) by rat liver microsomes was competitively inhibited by methimazole (MMI; 1-methyl-2-mercaptoimidazole), a known substrate and inhibitor of the microsomal FAD-containing monooxygenase. S-oxidation was also temporarily depressed in liver microsomes obtained from MMI-treated rats. When administered in vivo, MMI alleviated TB-induced liver necrosis in a dose-dependent manner; moreover, a significant decrease in the serum concentration of TBSO was observed. The protective effect of MMI against the necrogenic effect of TB could arise from competition of these two chemicals for the same bioactivating system, leading to a lower production of the liver damaging metabolite, TBSO.

Methimazole-induced modulation of thiobenzamide bioactivation and toxicity.

CHIELI, ELISABETTA;MALVALDI, GINO
1983

Abstract

The formation of thiobenzamide-S-oxide (TBSO) from thiobenzamide (TB) by rat liver microsomes was competitively inhibited by methimazole (MMI; 1-methyl-2-mercaptoimidazole), a known substrate and inhibitor of the microsomal FAD-containing monooxygenase. S-oxidation was also temporarily depressed in liver microsomes obtained from MMI-treated rats. When administered in vivo, MMI alleviated TB-induced liver necrosis in a dose-dependent manner; moreover, a significant decrease in the serum concentration of TBSO was observed. The protective effect of MMI against the necrogenic effect of TB could arise from competition of these two chemicals for the same bioactivating system, leading to a lower production of the liver damaging metabolite, TBSO.
Chieli, Elisabetta; Malvaldi, Gino
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/4743
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