Interaction of anticonvulsants with the barbiturate-benzodiazpine-gaba receptor complex

Frederik Leeb-Lundberg, Adele Snowman, Richard W. Olsen

Research output: Contribution to journalArticle

Abstract

Unlike the anesthetic barbiturate pentobarbital and the anxiolytic pyrazolopyridine etazolate, which enhance [3H]diazepam binding to rat brain membranes, the anticonvulsant barbiturates phenobarbital and metharbital, and also chlormethiazole, at therapeutic concentrations (10-1000 μM), do not stimulate [3H]diazepam binding, but instead block the enhancement by both pentobarbital and etazolate. The same anticonvulsants at similar concentrations inhibit [3H]α-dihydropicrotoxinin (DHP) binding, suggesting that these anticonvulsants compete for the same receptor sites as pentobarbital and etazolate, designated the barbiturate-picrotoxinin receptor component of the benzodiazepine-GABA receptor complex.

Original languageEnglish (US)
Pages (from-to)125-129
Number of pages5
JournalEuropean Journal of Pharmacology
Volume72
Issue number1
DOIs
StatePublished - Jun 10 1981

Keywords

  • Anesthetics
  • Anticonvulsants
  • Anxiolytics
  • Cl channels
  • γ-Aminobutyric acid

ASJC Scopus subject areas

  • Pharmacology

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