title: The benzodiazepine receptor ligand, methyl beta-carboline-3-carboxylate, is both sedative and proconvulsant in chicks.
abstract: Certain pharmacological properties of methyl beta-carboline-3-carboxylate (beta-CCM), a benzodiazepine receptor ligand, have been investigated in chicks. Although beta-CCM has been established previously as an "inverse agonist" of benzodiazepine receptors in rodents, having effects opposite to those of benzodiazepines in a variety of tests, in chicks this compound had a different pharmacological profile. Firstly, in contrast to the overt convulsant action of beta-CCM in other species, beta-CCM (0.05-40 mg/kg) did not produce convulsions by itself in chicks, but it was only proconvulsant. Secondly and most surprisingly, beta-CCM, like diazepam, produced in chicks a sedation which could be blocked by the benzodiazepine receptor antagonist Ro 15-1788. Thus it appears that beta-CCM can function both as an agonist and as an inverse agonist in this animal.
mesh_terms: D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology; D002243:Carbolines / Q000037:antagonists & inhibitors / Q000494:pharmacology* / Q000633:toxicity; D002645:Chickens; D003292:Convulsants / Q000037:antagonists & inhibitors / Q000494:pharmacology* / Q000633:toxicity; D005442:Flumazenil; D006993:Hypnotics and Sedatives / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D011963:Receptors, GABA-A / Q000187:drug effects*; D012640:Seizures / Q000139:chemically induced
chemical_list: D001570:Benzodiazepinones; D002243:Carbolines; D003292:Convulsants; D006993:Hypnotics and Sedatives; D011963:Receptors, GABA-A; C026072:1-methyl-beta-carboline-3-carboxylic acid; D005442:Flumazenil