Nutt D J, Lister R G
Laboratory of Clinical Studies, NIAAA, DICBR, Bethesda, MD 20892.
Eur J Pharmacol. 1989 Jun 8;165(1):135-8. doi: 10.1016/0014-2999(89)90779-6.
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.
评估了苯二氮䓬受体配体β-CMC（3-（甲氧基羰基）-氨基-β-咔啉）的内在效应及其与地西泮抗惊厥和镇静作用的相互作用。β-CMC（100毫克/千克腹腔注射）显著提高了对荷包牡丹碱的惊厥阈值。β-CMC（10毫克/千克）未能改变地西泮（5毫克/千克腹腔注射）的抗惊厥作用，但显著减弱了地西泮的镇静作用。更高剂量的β-CMC（40毫克/千克）确实减弱了地西泮的抗惊厥作用。数据表明β-CMC是苯二氮䓬受体的部分激动剂。
