Chweh A Y, Lin Y B, Swinyard E A
Life Sci. 1984 Apr 30;34(18):1763-8. doi: 10.1016/0024-3205(84)90576-9.
The objective of this investigation was to determine whether the effects of muscimol on benzodiazepine receptor binding relate to the hypnotic activity of nine benzodiazepines (clonazepam, triazolam, diazepam, flurazepam, nitrazepam, oxazepam, temazepam, clobazam, and chlordiazepoxide) and CL 218,872. There was no correlation between the basal receptor binding affinities of the drugs tested and their hypnotic potencies, whereas the benzodiazepine receptor agonists whose receptor bindings are strongly modulated by muscimol possess potent hypnotic activity. These results indicate that benzodiazepine receptors that couple to GABA receptors are involved in the hypnotic activity of the benzodiazepines.
本研究的目的是确定蝇蕈醇对苯二氮䓬受体结合的影响是否与九种苯二氮䓬类药物（氯硝西泮、三唑仑、地西泮、氟西泮、硝西泮、奥沙西泮、替马西泮、氯巴占和氯氮䓬）以及 CL 218,872 的催眠活性相关。所测试药物的基础受体结合亲和力与其催眠效力之间没有相关性，而其受体结合受到蝇蕈醇强烈调节的苯二氮䓬受体激动剂具有强效催眠活性。这些结果表明，与γ-氨基丁酸（GABA）受体偶联的苯二氮䓬受体参与了苯二氮䓬类药物的催眠活性。
