Hydroxylation of three benzodiazepines in vitro

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

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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
Issue number10
Publication statusPublished - 1977

ASJC Scopus subject areas

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


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