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The prethcamide hydroxylation system in rat hepatic microsomes


, : The prethcamide hydroxylation system in rat hepatic microsomes. Acta Biochimica Polonica 31(4): 409-420

Ethyl butamide and propyl butamide, the active constituents of the analeptic drug named Prethcamide (Ciba-Geigy), undergo biotransformation to respective single metabolites in the presence of rat hepatic microsomes and the NADPH-generating system. Spectral analysis showed that the metabolites were hydroxylated forms of the drug. The hydroxylation was stimulated by NADH and increased ionic strength, and inhibited by the known cytochrome P-450 inhibitors, e.g. SKF-525A [2-(diethylamino)ethyl-2,2-diphenylvalerate hydrochloride], metyrapone, CO and KCN. The drug formed type I binding spectrum with cytochrome P-450.

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