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依托唑啉或戊巴比妥增强的[³H]蝇蕈醇结合受苯二氮䓬激动剂和反向激动剂的差异调节。

Differential modulation of etazolate or pentobarbital enhanced [3H] muscimol binding by benzodiazepine agonists and inverse agonists.

作者信息

Borea P A, Supavilai P, Karobath M

出版信息

Brain Res. 1983 Dec 5;280(2):383-6. doi: 10.1016/0006-8993(83)90072-0.

Abstract

Flunitrazepam, a benzodiazepine agonist increases, and DMCM, an inverse agonist decreases the stimulation by etazolate or pentobarbital of [3H] muscimol binding to membranes of rat cerebral cortex. Ro 15-1788 has no marked effects but antagonizes the action of both flunitrazepam and DMCM. The investigation of several drugs acting on benzodiazepine receptors on etazolate enhancement of [3H] muscimol binding suggests that their receptor interaction reflects a spectrum from agonists to inverse agonists.

摘要

氟硝西泮,一种苯二氮䓬类激动剂,可增强[3H]蝇蕈醇与大鼠大脑皮层膜结合的作用,而DMCM,一种反向激动剂,则可减弱依托唑啉或戊巴比妥对其的刺激作用。Ro 15-1788无明显作用,但可拮抗氟硝西泮和DMCM的作用。对几种作用于苯二氮䓬受体的药物在依托唑啉增强[3H]蝇蕈醇结合方面的研究表明,它们与受体的相互作用反映了从激动剂到反向激动剂的一系列情况。

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