Prado de Carvalho L, Venault P, Potier M C, Dodd R H, Brown C L, Chapouthier G, Rossier J
Eur J Pharmacol. 1986 Oct 7;129(3):323-32. doi: 10.1016/0014-2999(86)90442-5.
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.
我们之前曾描述过一种新型化合物3-(甲氧基羰基)-氨基-β-咔啉（β-CMC）的合成，该化合物对苯二氮䓬受体具有较高的体外亲和力。体内试验表明，该化合物具有受限的药理特性。β-CMC缺乏内在活性，但它能拮抗β-咔啉-3-羧酸甲酯（一种苯二氮䓬受体反向激动剂）诱导的惊厥。此外，β-CMC能选择性拮抗苯二氮䓬类药物的镇静作用，但不拮抗其抗焦虑或抗惊厥作用。本文讨论了β-CMC对苯二氮䓬类药物镇静作用进行选择性拮抗可能涉及的机制。
