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Abstract
1. N-oxygenation of stobadine, a γ-carboline antiarrhythmic and cardioprotective agent, was investigated in vitro using rat liver preparations.
2. Stobadine N-oxygenase activity was located mainly in the microsomal fraction and exhibited a requirement for oxygen and NADPH. The apparent Km and Vmax values for the process were, respectively, 350 μ and 3.48nmol/mg protein per min.
3. N-oxygenation of stobadine in rat liver microsomes was not affected by SKF 525-A, carbon monoxide, metyrapone, cyanide or n-octylamine. When guinea-pig liver microsomes were used the reaction was activated by n-octylamine.
4. N-oxygenase activity was strongly inhibited by methimazole and depressed by phenobarbital and 3-methylcholantrene pretreatment.
5. The above results, along with the pH optimum of 8.4, strongly indicate the involvement of flavin-containing monooxygenase in the metabolic N-oxygenation of stobadine.
6. Species difference in liver microsomal N-oxygenase activity was evident, the order of activity being guinea-pig > rat > rabbit.