3-(Methoxycarbonyl)-amino-beta-carboline, a selective antagonist of the sedative effects of benzodiazepines.
We have previously described the synthesis of a novel compound, 3-(methoxycarbonyl)-amino-beta-carboline (beta-CMC), which has a high in vitro affinity for the benzodiazepine receptor. In vivo testing showed that this compound had a restricted pharmacological profile. beta-CMC lacked intrinsic activity but it antagonized the convulsions induced by the methyl ester of beta-carboline-3-carboxylic acid, an inverse agonist of the benzodiazepine receptor. Moreover, beta-CMC selectively antagonized the sedative but not the anxiolytic or anticonvulsant effects of benzodiazepines. The possible mechanisms involved in the selective antagonism of the sedative effects of benzodiazepines by beta-CMC are discussed.
D000818:Animals; D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001569:Benzodiazepines / Q000037:antagonists & inhibitors*; D002243:Carbolines / Q000494:pharmacology*; D006993:Hypnotics and Sedatives / Q000037:antagonists & inhibitors*; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D012640:Seizures / Q000188:drug therapy
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D002243:Carbolines; D006993:Hypnotics and Sedatives; D001569:Benzodiazepines; C051027:3-(methoxycarbonyl)amino-beta-carboline