Antagonism of flurazepam and other effects of Ro15-1788, PK8165 and Ro5-4864 on the GABA-A receptor complex in rat cuneate nucleus

Eur J Pharmacol. 1985 Oct 29;117(1):51-60. doi: 10.1016/0014-2999(85)90471-6.

Abstract

In slices of rat cuneate nucleus, responses to the GABA-A receptor agonist muscimol were potentiated by flurazepam. The maximal potentiation by 1 microM flurazepam was antagonized by the neuronal benzodiazepine receptor ligand Ro15-1788 3 microM, by the quinoline derivative PK8165 0.1 microM and by the peripheral-type benzodiazepine receptor ligand Ro5-4864 0.1 microM. Another ligand for the peripheral-type benzodiazepine receptor, PK11195 10 microM, enhanced the potentiating effect of a submaximal concentration of flurazepam 0.1 microM and prevented the antagonism of flurazepam by Ro5-4864. At much higher concentrations of these drugs, additional effects were seen. Ro15-1788 30 microM and PK11195 30 microM each caused small potentiations of muscimol while Ro5-4864 30 microM caused a small antagonism. Ro15-1788 30 microM, PK8165 100 microM and Ro5-4864 30 microM all antagonized the potentiation of muscimol by pentobarbitone 10 microM; also, PK8165 and Ro5-4864 enhanced the potency of picrotoxin as an antagonist of muscimol. It is concluded that both Ro5-4864 and PK8165 have several distinct effects on the GABA-A receptor complex, all of which could result in reduced responses to muscimol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / pharmacology*
  • Benzodiazepinones / pharmacology
  • Drug Synergism
  • Flumazenil
  • Flurazepam / antagonists & inhibitors*
  • In Vitro Techniques
  • Male
  • Medulla Oblongata / drug effects
  • Medulla Oblongata / metabolism*
  • Muscimol
  • Pentobarbital / pharmacology
  • Picrotoxin / pharmacology
  • Quinolines / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / drug effects*

Substances

  • Anticonvulsants
  • Benzodiazepinones
  • Quinolines
  • Receptors, GABA-A
  • Picrotoxin
  • Muscimol
  • 4'-chlorodiazepam
  • Flumazenil
  • Pentobarbital
  • Flurazepam
  • pipequaline