Octoclothepine-N-oxide is reduced to octoclothepine by rat liver microsomes in the presence of NADPH under anaerobic conditions. Carbon monoxide and oxygen inhibit this reaction. SKF 525A slightly stimulated the reduction rate of octoclothepine-N-oxide. Kinetic data for this enzymic reduction suggest a high affinity of the microsomal enzyme system toward the N-oxide. This biotransformation reaction may represent a mechanism for regulation of drug level in patients.
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