Pharmacology of methyl- and propyl-beta-carbolines in a hereditary model of epilepsy.
Intravenous administration of beta-carboline-3-carboxylate methyl ester (beta-CCM) produced convulsions at small doses (0.03 mg/kg) in adult chickens, homozygous for the epileptic gene. Nonepileptic heterozygote hatchmates (carriers) did not undergo seizures at doses of 1 mg/kg, and doses of 3-5 mg/kg produced only brief myoclonic responses. The convulsant effect of beta-CCM could be prevented by pretreatment with large doses of beta-carboline-3-carboxylate propyl ester (beta-CCP). beta-Carboline-3-carboxylate methyl ester displayed a higher affinity than diazepam in displacement studies on synaptosomal membrane preparations from brains of epileptic and carrier chickens.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000494:pharmacology*; D002243:Carbolines / Q000494:pharmacology*; D002645:Chickens; D003292:Convulsants / Q000494:pharmacology*; D003975:Diazepam / Q000378:metabolism; D004827:Epilepsy / Q000235:genetics / Q000503:physiopathology*; D006579:Heterozygote; D006720:Homozygote; D007211:Indoles / Q000494:pharmacology*; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D002243:Carbolines; D003292:Convulsants; D007211:Indoles; D011963:Receptors, GABA-A; C028585:propyl beta-carboline-3-carboxylate; C036150:beta-carboline-3-carboxylic acid methyl ester; D003975:Diazepam