Benzodiazepine anticonvulsants accelerate and beta-carboline convulsants decelerate the kinetics of [35S]TBPS binding at the chloride ionophore

Eur J Pharmacol. 1985 Nov 5;117(2):275-8. doi: 10.1016/0014-2999(85)90614-4.

Abstract

The effect of flunitrazepam and DMCM was examined on the kinetics of [35S]t-butylbicyclophosphorothionate (TBPS) binding. The enhancing effect of flunitrazepam and the decreasing effect of DMCM on TBPS binding was due to non-equilibrium conditions. The anticonvulsant benzodiazepine increased both the association and dissociation rate constants. The convulsant beta-carboline had the opposite effect. Benzodiazepine receptor ligands might affect the convulsant TBPS sites parallel with opening/closing of the chloride ionophores.

MeSH terms

  • Animals
  • Anticonvulsants / pharmacology*
  • Benzodiazepines / pharmacology*
  • Bridged Bicyclo Compounds / metabolism*
  • Bridged Bicyclo Compounds, Heterocyclic*
  • Bridged-Ring Compounds / metabolism*
  • Carbolines / pharmacology*
  • Chlorides / metabolism*
  • Convulsants / pharmacology*
  • Flunitrazepam / pharmacology
  • In Vitro Techniques
  • Ionophores / metabolism*
  • Male
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / drug effects
  • Synaptic Membranes / metabolism

Substances

  • Anticonvulsants
  • Bridged Bicyclo Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Bridged-Ring Compounds
  • Carbolines
  • Chlorides
  • Convulsants
  • Ionophores
  • Receptors, GABA-A
  • Benzodiazepines
  • methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate
  • Flunitrazepam
  • tert-butylbicyclophosphorothionate