A study on the Prethcamide hydroxylation system in rat hepatic microsomes.
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.
D000613:Aminobutyrates / Q000378:metabolism*; D000818:Animals; D001711:Biotransformation; D002849:Chromatography, Gas; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D006863:Hydrogen-Ion Concentration; D006900:Hydroxylation; D007700:Kinetics; D008297:Male; D008862:Microsomes, Liver / Q000201:enzymology*; D009243:NAD / Q000494:pharmacology; D009249:NADP / Q000378:metabolism / Q000494:pharmacology; D051381:Rats
D000613:Aminobutyrates; D065607:Cytochrome P-450 Enzyme Inhibitors; D009243:NAD; C100196:prethcamide; D009249:NADP; D003577:Cytochrome P-450 Enzyme System