苯二氮䓬受体配体β-咔啉-3-羧酸甲酯在雏鸡中既有镇静作用又有惊厥作用。

The benzodiazepine receptor ligand, methyl beta-carboline-3-carboxylate, is both sedative and proconvulsant in chicks.

作者信息

Venault P, Prado de Carvalho L, Brown C L, Dodd R H, Rossier J, Chapouthier G

出版信息

Life Sci. 1986 Sep 22;39(12):1093-100. doi: 10.1016/0024-3205(86)90201-8.

Abstract

Certain pharmacological properties of methyl beta-carboline-3-carboxylate (beta-CCM), a benzodiazepine receptor ligand, have been investigated in chicks. Although beta-CCM has been established previously as an "inverse agonist" of benzodiazepine receptors in rodents, having effects opposite to those of benzodiazepines in a variety of tests, in chicks this compound had a different pharmacological profile. Firstly, in contrast to the overt convulsant action of beta-CCM in other species, beta-CCM (0.05-40 mg/kg) did not produce convulsions by itself in chicks, but it was only proconvulsant. Secondly and most surprisingly, beta-CCM, like diazepam, produced in chicks a sedation which could be blocked by the benzodiazepine receptor antagonist Ro 15-1788. Thus it appears that beta-CCM can function both as an agonist and as an inverse agonist in this animal.

摘要

已在雏鸡中研究了苯二氮䓬受体配体β-咔啉-3-羧酸甲酯（β-CCM）的某些药理学特性。尽管β-CCM先前已被确定为啮齿动物中苯二氮䓬受体的“反向激动剂”，在各种测试中其作用与苯二氮䓬相反，但在雏鸡中该化合物具有不同的药理学特征。首先，与β-CCM在其他物种中明显的惊厥作用相反，β-CCM（0.05-40mg/kg）本身在雏鸡中不会产生惊厥，而只是促惊厥作用。其次且最令人惊讶的是，β-CCM与地西泮一样，在雏鸡中产生镇静作用，该作用可被苯二氮䓬受体拮抗剂Ro 15-1788阻断。因此，在这种动物中，β-CCM似乎既可以作为激动剂也可以作为反向激动剂发挥作用。