Oxazepam Esters. 3. Intrinsic Activity, Selectivity, and Prodrug Effect

Gábor Maksay, Eva Pálosi, Zsuzsanna Tegyey, László Ótvós

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Antimetrazol and muscle-relaxant activities of 11 aliphatic esters of oxazepam were studied as a function of time in mice. The esters given intravenously retained antimetrazol activity, while muscle-relaxant activity was generally decreased. The administration of a dose equivalent to the antimetrazol EDgo resulted in constant oxazepam brain levels for most esters; therefore, the intrinsic anticonvulsant activity of the intact ester is insignificant. The dimethylphenylpropionyl ester appeared to antagonize the effect of oxazepam, since it elevated the free oxazepam level required to achieve the EDgo in the antimetrazol assay. The administration of doses equivalent to the muscle-relaxant EDgo values resulted in no correlation with total brain benzodiazepine levels, suggesting that changes in the selectivity of action are the consequence of different sites of action.

Original languageEnglish
Pages (from-to)499-502
Number of pages4
JournalJournal of Medicinal Chemistry
Volume24
Issue number5
DOIs
Publication statusPublished - May 1981

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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