人类大脑中的苯二氮䓬受体：特性、亚细胞定位及增溶作用。

Benzodiazepine receptors in human brain: characterization, subcellular localization and solubilization.

Maloteaux J M, Octave J N, Vanisberg M A, Kollmann P, Ackermans A, Laterre C

Université Catholique de Louvain, Laboratoire de Neurochimie Brussels, Belgium.

Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(5):773-82. doi: 10.1016/0278-5846(88)90022-x.

Abstract

Benzodiazepine receptors have been characterized in human brain mainly using [3H]-Ro 15-1788 and [3H]-flunitrazepam. Both ligands present a very high affinity for the receptor sites (Kd values of 0.56 and 1.53 nM respectively). 2. GABA enhanced the affinity of [3H]-flunitrazepam and [3H]-diazepam, but not that of [3H]-Ro 15-1788 and [3H]-methyl-beta-carboline 3-carboxylate for their specific binding sites as well in cerebral as in cerebellar human cortex. 3. Subcellular distribution of the benzodiazepine receptors revealed a main synaptosomal localization in human cerebral cortex, cerebellum and striatum. 4. Solubilized benzodiazepine receptors were obtained using 0.5% sodium deoxycholate and were characterized with [3H]-Ro 15-1788. The solubilized receptors are still coupled to GABA receptors since the [3H]-flunitrazepam specific binding was enhanced in the presence of micromolar concentrations of GABA.

摘要

苯二氮䓬受体主要通过使用[3H]-Ro 15-1788和[3H]-氟硝西泮在人脑中进行了表征。两种配体对受体位点都具有非常高的亲和力（Kd值分别为0.56和1.53 nM）。2. γ-氨基丁酸（GABA）增强了[3H]-氟硝西泮和[3H]-地西泮的亲和力，但在人脑皮质和小脑皮质中，对[3H]-Ro 15-1788和[3H]-甲基-β-咔啉-3-羧酸对其特异性结合位点的亲和力没有增强作用。3. 苯二氮䓬受体的亚细胞分布显示在人脑海马、小脑和纹状体中主要定位于突触体。4. 使用0.5%脱氧胆酸钠获得了可溶的苯二氮䓬受体，并用[3H]-Ro 15-1788对其进行了表征。由于在微摩尔浓度的GABA存在下[3H]-氟硝西泮特异性结合增强，所以可溶受体仍与GABA受体偶联。