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- W2338960127 abstract "The metabolism of the anthelmintic nitroheterocyclic compound niridazole by rat liver was studied under aerobic conditions in vitro . Metabolism was localized to the microsomal fraction. Four metabolites of niridazole were isolated from these microsomal systems by high pressure liquid chromatography. The metabolites were characterized by mass spectrometry and 1 H Fourier transform nuclear magnetic resonance spectroscopy as the 4-hydroxy, 5-hydroxy, 4,5-dihydroxy and the 4,5-dehydro derivatives of the imidazolidinone ring; the nitrothiazole portion of niridazole apparently was unaltered. The aerobic metabolism was shown to require O 2 and exogenous reducing equivalents (NADPH was more effective than NADH), and to be inhibited by CO, suggesting a cytochrome P-450 catalyzed reaction. Inducers of microsomal cytochrome P-450, phenobarbital and 3-methylcholanthrene, were found to enhance niridazole metabolism. Metabolite profiles varied quantitatively with different inducers. Experiments with individual aerobic metabolites showed precursor-product relationships that are consistent with formation of an epoxide intermediate in the overall metabolic sequence." @default.
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- W2338960127 date "1979-11-01" @default.
- W2338960127 modified "2023-09-23" @default.
- W2338960127 title "Aerobic metabolism of niridazole by rat liver microsomes." @default.
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