γ-氨基丁酸（GABA）和苯二氮䓬拮抗剂对[³H]氟硝西泮与大脑皮质膜结合的影响。

Effect of GABA and benzodiazepine antagonists on [3H]flunitrazepam binding to cerebral cortical membrane.

作者信息

Fong J, Okada K, Lew J Y, Goldstein M

出版信息

Brain Res. 1983 Apr 25;266(1):152-4. doi: 10.1016/0006-8993(83)91319-7.

Abstract

The effects of GABA on the binding of [3H]flunitrazepam to bovine cerebral cortical membranes was investigated in presence and in absence of benzodiazepine antagonists. The percentage stimulation of [3H]flunitrazepam binding by GABA is higher when approximately 50% of the binding is displaced by benzodiazepine antagonists. The observed increase in percent stimulation of [3H]flunitrazepam binding by GABA might reflect the preferential displacement of the ligand by benzodiazepine antagonists from a GABA-insensitive conformational state or site of the receptor.

摘要

在存在和不存在苯二氮䓬拮抗剂的情况下，研究了γ-氨基丁酸（GABA）对[3H]氟硝西泮与牛脑皮质膜结合的影响。当约50%的结合被苯二氮䓬拮抗剂取代时，GABA对[3H]氟硝西泮结合的刺激百分比更高。观察到的GABA对[3H]氟硝西泮结合刺激百分比的增加可能反映了苯二氮䓬拮抗剂将配体从受体的GABA不敏感构象状态或位点优先取代。