两种苯二氮䓬受体的物理分离与特性鉴定
Physical separation and characterization of two types of benzodiazepine receptors.
作者信息
Lo M M, Strittmatter S M, Snyder S H
出版信息
Proc Natl Acad Sci U S A. 1982 Jan;79(2):680-4. doi: 10.1073/pnas.79.2.680.
Abstract
Two distinct benzodiazepine receptors are solubilized differentially by various detergents. The receptor sites that resist solubilization, designated type I, are most highly concentrated in the cerebellum and corpus striatum whereas the more readily solubilized receptors, type II, are most enriched in the hippocampus. The type I receptors display higher affinity for beta-carboline esters and a triazolopyridazine whereas several benzodiazepines do not differentiate the two receptors. The type I receptors can be solubilized with 2% Triton X-100/1 M NaCl; they retain the same drug specificity as in the particulate state.
摘要
两种不同的苯二氮䓬受体可被各种去污剂不同程度地溶解。抗溶解的受体位点（称为I型）在小脑和纹状体中浓度最高，而较易溶解的受体（II型）在海马体中最为丰富。I型受体对β-咔啉酯和三唑并哒嗪显示出更高的亲和力，而几种苯二氮䓬类药物无法区分这两种受体。I型受体可用2% Triton X-100/1 M NaCl溶解；它们保留了与颗粒状态相同的药物特异性。
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