3-(Methoxycarbonyl)-amino-beta-carboline reduces both the sedative and anticonvulsant effects of diazepam.
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.
Nutt
D J
DJ
Laboratory of Clinical Studies, NIAAA, DICBR, Bethesda, MD 20892.
Lister
R G
RG
D000818:Animals; D000927:Anticonvulsants / Q000037:antagonists & inhibitors*; D001640:Bicuculline / Q000494:pharmacology; D002243:Carbolines / Q000494:pharmacology*; D003975:Diazepam / Q000037:antagonists & inhibitors*; D006993:Hypnotics and Sedatives / Q000037:antagonists & inhibitors*; D008297:Male; D051379:Mice; D012640:Seizures / Q000503:physiopathology; D013997:Time Factors
D000927:Anticonvulsants; D002243:Carbolines; D006993:Hypnotics and Sedatives; C051027:3-(methoxycarbonyl)amino-beta-carboline; D003975:Diazepam; D001640:Bicuculline