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1960年利眠宁始用于临床、二十多年来利眠宁、安定等苯二氮(BDZ)类药物在临床上广泛使用。它们具有抗焦虑、抗惊厥、抗癫痫、抗室性心律失常、以及镇静、催眠和肌肉松弛等效应。1977年Squires小组和Mohler小组几乎同时报道大鼠中枢神经组织存在BDZ的高亲和力,可饱和特异结合部位,BDZ类药物与之结合的亲和力和它们对猫肌肉的松弛效力之间存在良好相关性,从而指出体内存在BDZ受体。近年来BDZ受体已成为分子药理学中一个十分活跃的研究领域。本文主要介绍BDZ受体与γ-氨基丁酸(GABA)受体的关系。在BDZ受体的概念提出之前,已发现
Sheletianning began to be used in clinic in 1960, and benzodiazepine (BDZ) was widely used clinically for more than two decades. They have anti-anxiety, anticonvulsant, anti-epilepsy, anti-ventricular arrhythmia, and sedation, hypnosis and muscle relaxation and other effects. In 1977, the Squires group and the Mohler group reported almost simultaneously that there was a high affinity and saturable specific binding site of BDZ in the central nervous system of rats. There was a good correlation between the affinity of BDZ-type drugs and their relaxing effect on the cat muscles, Indicating that BDZ receptors are present in the body. In recent years, BDZ receptor has become a very active research field in molecular pharmacology. This article describes the BDZ receptor and γ-aminobutyric acid (GABA) receptor relationship. It has been found before the concept of BDZ receptor is proposed