title: Hydroxylation of three benzodiazepines in vitro.
abstract: Three structurally related benzodiazepines were studied as substrates for hydroxylation by liver microsomal enzymes of rats and mice. The Vmax was comparable for dechlorodesmethyldiazepam, desmethyldiazepam, and 2'-chlorodesmethyldiazepam in the two animal species. The apparent Km decreased from dechlorodesmethyldiazepam to 2'-chlorodesmethyldiazepam for liver microsomal enzymes from both animal species. The hydroxylation of desmethyldiazepam and 2'-chlorodesmethyldiazepam yielded two pharmacologically active metabolites, oxazepam and lorazepam, respectively.
mesh_terms: D000818:Animals; D001711:Biotransformation; D003975:Diazepam / Q000031:analogs & derivatives*; D006900:Hydroxylation; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D003708:Nordazepam / Q000031:analogs & derivatives* / Q000378:metabolism*; D051381:Rats
chemical_list: D003708:Nordazepam; D003975:Diazepam