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A study on the Prethcamide hydroxylation system in rat hepatic microsomes.

Tadeusz Szumiło, Piotr Bryła, A Byra

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Abstract

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, metyrapone, CO and KCN. The drug formed type I binding spectrum with cytochrome P-450.

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What this paper is about

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, metyrapone, CO and KCN. The drug formed type I binding spectrum with cytochrome P-450.

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Available abstract

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, metyrapone, CO and KCN. The drug formed type I binding spectrum with cytochrome P-450.

Key concepts: Hydroxylation, Microsome, Chemistry, Cytochrome, Biotransformation, Microsoma, Metyrapone, Cytochrome P450

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A study on the Prethcamide hydroxylation system in rat hepatic microsomes. — Research Paper | ScholarLens