Kawasaki K, Kodama M, Matsushita A
Eur J Pharmacol. 1984 Jun 15;102(1):147-50. doi: 10.1016/0014-2999(84)90348-0.
The antagonistic and intrinsic activity of an imidazodiazepine derivative, Ro 15-1788, was manifested on the crossed extensor reflex. Ro 15-1788 antagonized the depressant effect of diazepam and shifted the dose-response curve of diazepam to the right in a parallel manner but could not reverse the depression produced by either phenobarbital or chlorpromazine. Ro 15-1788 also antagonized the enhancement produced by ethyl-beta-carboline-3-carboxylate. When administered alone, Ro 15-1788 showed a weak depressant effect. Thus, Ro 15-1788 seems to be a partial agonist on the benzodiazepine receptors with weak intrinsic activity and pharmacological properties differing from those of ethyl-beta-carboline-3-carboxylate.
一种咪唑二氮卓衍生物Ro 15 - 1788的拮抗和内在活性在交叉伸肌反射中得以体现。Ro 15 - 1788拮抗地西泮的抑制作用，并使地西泮的剂量 - 反应曲线平行右移，但不能逆转苯巴比妥或氯丙嗪所产生的抑制作用。Ro 15 - 1788还拮抗β - 咔啉 - 3 - 羧酸乙酯所产生的增强作用。单独给药时，Ro 15 - 1788表现出微弱的抑制作用。因此，Ro 15 - 1788似乎是苯二氮卓受体上的部分激动剂，内在活性较弱，其药理特性与β - 咔啉 - 3 - 羧酸乙酯不同。
