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人类小脑皮质中的苯二氮䓬受体:一项定量放射自显影和药理学研究,证明I型受体占主导地位。

Benzodiazepine receptors in the human cerebellar cortex: a quantitative autoradiographic and pharmacological study demonstrating the predominance of type I receptors.

作者信息

Faull R L, Villiger J W, Holford N H

出版信息

Brain Res. 1987 May 19;411(2):379-85. doi: 10.1016/0006-8993(87)91091-2.

DOI:10.1016/0006-8993(87)91091-2
PMID:3038261
Abstract

The anatomical localization of benzodiazepine receptors in the human cerebellar cortex was studied using quantitative autoradiography following in vitro labelling of cryostat sections with [3H]flunitrazepam ([3H]FNZ), and the pharmacology of these receptors has been characterized by computerized, non-linear least squares regression analysis of [3H]FNZ displacement by FNZ, CL218,872 and ethyl beta-carboline-3-carboxylate (ECC) binding to membranes. The autoradiograms demonstrated that benzodiazepine receptors were present throughout all layers of the human cerebellar cortex; high concentrations of receptors were present in the molecular layer, moderate concentrations were present in the granular layer and a much lower density of receptors was seen in the intervening Purkinje cell layer. The pharmacological studies indicated that the human cerebellar cortex contained a high concentration of homogeneous benzodiazepine receptors which have high affinity for FNZ, ECC and CL218,872, i.e. type I sites.

摘要

使用[3H]氟硝西泮([3H]FNZ)对冰冻切片进行体外标记后,通过定量放射自显影术研究了苯二氮䓬受体在人类小脑皮质中的解剖定位,并且通过对FNZ、CL218,872和β-咔啉-3-羧酸乙酯(ECC)与膜结合导致的[3H]FNZ位移进行计算机化非线性最小二乘回归分析,对这些受体的药理学特性进行了表征。放射自显影片显示,苯二氮䓬受体存在于人类小脑皮质的所有层中;分子层中存在高浓度的受体,颗粒层中存在中等浓度的受体,而介于其间的浦肯野细胞层中受体密度则低得多。药理学研究表明,人类小脑皮质含有高浓度的同质性苯二氮䓬受体,这些受体对FNZ、ECC和CL218,872具有高亲和力,即I型位点。

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