Modulation of benzodiazepine receptor binding: Insight into pharmacological efficacy

Frederick J. Ehlert, Paul Ragan, Andrew Chen, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticle

47 Scopus citations

Abstract

The effects of GABA on the binding of analogues of benzodiazepine, triazolopyridazines, β-carbolines and imidazodiazepines were examined in ligand/[3H]flunitrazepan competition experiments. GABA increased the potency of anxiolytics, like flunitrazepam, whereas the potency of benzodiazepine antagonists, like Ro15-1788, was largely insensitive to the influence of GABA. Several other agents including pyrazolopyridines, barbiturates and etomidate caused a chloride dependent enhancement of [3H]flunitrazepam binding but not an enhancement of [3H]propyl-β-carboline-3-carboxylate binding.

Original languageEnglish (US)
Pages (from-to)249-253
Number of pages5
JournalEuropean Journal of Pharmacology
Volume78
Issue number2
DOIs
StatePublished - Feb 26 1982
Externally publishedYes

Keywords

  • Barbiturates
  • Benzodiazepine receptor agonists and antagonists
  • Etomidate
  • GABA
  • Pyrazolopyridines

ASJC Scopus subject areas

  • Pharmacology

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