3-(Methoxycarbonyl)-amino-beta-carboline reduces both the sedative and anticonvulsant effects of diazepam

Eur J Pharmacol. 1989 Jun 8;165(1):135-8. doi: 10.1016/0014-2999(89)90779-6.

Abstract

The intrinsic effects of the benzodiazepine receptor ligand beta-CMC (3-(methoxycarbonyl)-amino-beta-carboline) and its interaction with the anticonvulsant and sedative effects of diazepam were assessed. beta-CMC (100 mg/kg i.p.) significantly elevated seizure threshold to bicuculline. beta-CMC (10 mg/kg) failed to alter the anticonvulsant action of diazepam (5 mg/kg i.p.), but significantly attenuated diazepam's sedative effect. A higher dose of beta-CMC (40 mg/kg) did attenuate diazepam's anticonvulsant action. The data suggest that beta-CMC is a partial agonist at benzodiazepine receptors.

MeSH terms

  • Animals
  • Anticonvulsants / antagonists & inhibitors*
  • Bicuculline / pharmacology
  • Carbolines / pharmacology*
  • Diazepam / antagonists & inhibitors*
  • Hypnotics and Sedatives / antagonists & inhibitors*
  • Male
  • Mice
  • Seizures / physiopathology
  • Time Factors

Substances

  • Anticonvulsants
  • Carbolines
  • Hypnotics and Sedatives
  • 3-(methoxycarbonyl)amino-beta-carboline
  • Diazepam
  • Bicuculline