Modulation of benzodiazepine receptor binding: insight into pharmacological efficacy

Eur J Pharmacol. 1982 Feb 26;78(2):249-53. doi: 10.1016/0014-2999(82)90246-1.

Abstract

The effects of GABA on the binding of analogues of benzodiazepines, triazolopyridazines, beta-carbolines and imidazodiazepines were examined in ligand/[3H] flunitrazepam 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-beta-carboline-3-carboxylate binding.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding, Competitive
  • Cerebral Cortex / metabolism
  • In Vitro Techniques
  • Ligands
  • Rats
  • Receptors, Drug / drug effects
  • Receptors, Drug / metabolism*
  • Receptors, GABA-A
  • gamma-Aminobutyric Acid / pharmacology*

Substances

  • Ligands
  • Receptors, Drug
  • Receptors, GABA-A
  • gamma-Aminobutyric Acid