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苯二氮䓬类部分激动剂Ro16 - 6028和Ro17 - 1812可增加未禁食大鼠对美味食物的摄入量。

The benzodiazepine partial agonists, Ro16-6028 and Ro17-1812, increase palatable food consumption in nondeprived rats.

作者信息

Yerbury R E, Cooper S J

机构信息

Department of Psychology, University of Birmingham, U.K.

出版信息

Pharmacol Biochem Behav. 1987 Dec;28(4):427-31. doi: 10.1016/0091-3057(87)90500-4.

Abstract

Two novel imidazobenzodiazepines, Ro16-6028 and Ro17-1812, have been described recently as partial agonists acting at benzodiazepine receptors. In a test of palatable food consumption using nondeprived rats, Ro16-6028 (0.01-10 mg/kg) and Ro17-1812 (0.01-10 mg/kg) were shown to produce dose-dependent increases in food intake. Ro16-6028 was more potent than Ro17-1812. Suriclone, midazolam, and the beta-carbolines ZK 93423 and ZK 91296 also significantly increased food intake. The maximum effects of Ro16-6028 and Ro17-1812 were at least equivalent to those obtained with full agonists acting at benzodiazepine sites. Neither Ro16-6028 nor Ro17-1812 reduced locomotion or rearing frequency in an open field test, although there was a reduction in grooming frequency. In contrast, the full agonist midazolam dose-dependently reduced all measures of general activity. The results indicate that some novel benzodiazepine partial agonists strongly stimulate food intake in the absence of side effects typical of the classical benzodiazepines.

摘要

最近有两种新型咪唑并苯二氮䓬类药物,Ro16 - 6028和Ro17 - 1812,被描述为作用于苯二氮䓬受体的部分激动剂。在一项使用未禁食大鼠的可口食物消耗测试中,Ro16 - 6028(0.01 - 10毫克/千克)和Ro17 - 1812(0.01 - 10毫克/千克)显示出能使食物摄入量呈剂量依赖性增加。Ro16 - 6028比Ro17 - 1812更有效。舒立克隆、咪达唑仑以及β - 咔啉类药物ZK 93423和ZK 91296也显著增加了食物摄入量。Ro16 - 6028和Ro17 - 1812的最大效应至少等同于作用于苯二氮䓬位点的完全激动剂所产生的效应。在旷场试验中,Ro16 - 6028和Ro17 - 1812均未降低运动或竖毛频率,不过梳理频率有所降低。相比之下,完全激动剂咪达唑仑能剂量依赖性地降低所有一般活动指标。结果表明,一些新型苯二氮䓬类部分激动剂在没有经典苯二氮䓬类典型副作用的情况下能强烈刺激食物摄入。

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