Antagonism of benzodiazepine binding in rat and human brain by antiliriumR

K. V. Speeg, Sherry Wang, George R. Avant, M. Lawrence Berman, Steven Schenker

Research output: Contribution to journalArticle

9 Scopus citations

Abstract

Physostigmine (AntiliriumR) has been reported to reverse benzodiazepine- induced sleep or coma in man and prevent death in animals. Accordingly, we investigated the effect of Antilirium upon benzodiazepine binding to both rat and human brain. We report that Antilirium inhibits 3H-diazepam and 3H-flunitrazepam binding in a dose-dependent manner. The degree of inhibition of binding by Antilirium correlates with the affinity of benzodiazepine for its "receptor" such that diazepam is more affected than flunitrazepam. The inhibition is rapid but the kinetics are complex with only doses of Antilirium showing competitive inhibition when studied at equilibrium. These results may explain, at least in part, the effectiveness of Antilirium at reversing benzodiazepine-induced hypnosis without necessarily implicating a cholinergic mechanism.

Original languageEnglish (US)
Pages (from-to)1345-1350
Number of pages6
JournalLife Sciences
Volume24
Issue number15
DOIs
StatePublished - Apr 9 1979

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ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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