Hydroxylation of three benzodiazepines in vitro

E. Mussini, F. Marcucci, L. Airoldi, T. Facchinetti, S. Garattini

Research output: Contribution to journalArticlepeer-review

Abstract

Three structurally related benzodiazepines were studied as substrates for hydroxylation by liver microsomal enzymes of rats and mice. The V(max) was comparable for dechlorodesmethyldiazepam, desmethyldiazepam, and 2' chlorodesmethyldiazepam in the 2 animal species. The apparent K(m) decreased from dechlorodesmethyldiazepam to 2' chlorodesmethyldiazepam for liver microsomal enzymes from both animal species. The hydroxylation of desmethyldiazepam and 2' chlorodesmethyldiazepam yielded 2 pharmacologically active metabolites, oxazepam and lorazepam, respectively.

Original languageEnglish
Pages (from-to)1482-1483
Number of pages2
JournalJournal of Pharmaceutical Sciences
Volume66
Issue number10
Publication statusPublished - 1977

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

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