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新型喹啉衍生物系列在苯二氮䓬受体上的激动剂和拮抗剂活性。

Agonist and antagonist activities at benzodiazepine receptors of a novel series of quinoline derivatives.

作者信息

Gardner C R, Deacon R, James V, Parker F, Budhram P

机构信息

Roussel Laboratories Limited, Covingham, Swindon, Wiltshire, U.K.

出版信息

Eur J Pharmacol. 1987 Oct 13;142(2):285-95. doi: 10.1016/0014-2999(87)90118-x.

DOI:10.1016/0014-2999(87)90118-x
PMID:2826181
Abstract

Five members of a novel series of quinoline derivatives which all have similar activities on benzodiazepine receptor binding in vitro were compared in a food-motivated conflict and stress-induced ultrasounds models of anxiety and on suprahyoid muscle twitching in urethane-anaesthetised rats. RU 42382, RU 43028 and RU 39419 showed anxiolytic activity in both tests and RU 40410 was an antagonist. RU 40744 inhibited stress-induced ultrasounds but had little activity in the conflict test. Amphetamine-induced suprahyoid muscle twitching was only weakly inhibited by RU 42382 and RU 43028 in comparison with a classical benzodiazepine agonist. Ro15-1788 antagonised RU 42382 indicating that a major component of its action was agonism at benzodiazepine receptors. RU 39419 had no effect, RU 40744 tended to increase and RU 40410 evoked a small but statistically significant increase in twitching. The same rank order was observed in antagonism of a benzodiazepine in the muscle twitching model. RU 42382 was least effective as an antagonist and RU 40410 most effective. RU 39419 had no effect alone but antagonised the decrease of firing rate of cerebellar Purkinje cells induced by a benzodiazepine in urethane-anaesthetised rats. Comparison of in vivo occupancy of benzodiazepine receptors and efficacy in the conflict test in rats suggests a ranking of agonist intrinsic activity: RU 42382 greater than RU 43028 greater than RU 39419. A simple relationship between intrinsic activity at benzodiazepine receptors and structure of the compounds is proposed.

摘要

在食物诱导冲突和应激诱导超声焦虑模型以及乌拉坦麻醉大鼠的舌骨上肌群抽搐实验中，比较了一系列新型喹啉衍生物中的五个成员，它们在体外对苯二氮䓬受体结合均具有相似活性。RU 42382、RU 43028和RU 39419在两项实验中均显示出抗焦虑活性，而RU 40410是拮抗剂。RU 40744可抑制应激诱导的超声，但在冲突实验中活性很小。与经典苯二氮䓬激动剂相比，苯丙胺诱导的舌骨上肌群抽搐仅被RU 42382和RU 43028微弱抑制。Ro15 - 1788拮抗RU 42382，表明其作用的主要成分是对苯二氮䓬受体的激动作用。RU 39419无作用，RU 40744有增加趋势，而RU 40410引起轻微但具有统计学意义的抽搐增加。在肌肉抽搐模型中拮抗苯二氮䓬时也观察到相同的顺序。RU 42382作为拮抗剂效果最差，而RU 40410最有效。RU 39419单独无作用，但拮抗乌拉坦麻醉大鼠中苯二氮䓬诱导的小脑浦肯野细胞放电频率降低。大鼠体内苯二氮䓬受体占有率与冲突实验中疗效的比较表明激动剂内在活性的排序为：RU 42382大于RU 43028大于RU 39419。提出了苯二氮䓬受体内在活性与化合物结构之间的简单关系。

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