Braestrup C, Squires R F
Br J Psychiatry. 1978 Sep;133:249-60. doi: 10.1192/bjp.133.3.249.
Brain membranes from rat and human contain a single class of brain specific binding sites for pharmacologically and clinically active benzodiazepines. There is good correlation between the pharmacological effects of benzodiazepines and the affinity for the 3H-diazepam binding site. Benzodiazepine binding sites are not present on glial cells. Selective neuronal degeneration experiments in rats indicate a neuronal localization. 3H-Flunitrazepam is a very suitable ligand for affinity binding and it binds to the same class of binding sites as 3H-diazepam. Our results indicate that the in vitro 3H-diazepam and 3H-flunitrazepam binding sites are the receptors which in vivo mediate various pharmacological and clinical effects of benzodiazepines.
大鼠和人类的脑膜含有一类单一的、对药理和临床活性苯二氮䓬具有脑特异性的结合位点。苯二氮䓬的药理作用与其对³H-地西泮结合位点的亲和力之间存在良好的相关性。苯二氮䓬结合位点不存在于神经胶质细胞上。大鼠的选择性神经元变性实验表明其定位于神经元。³H-氟硝西泮是一种非常适合用于亲和结合的配体，它与³H-地西泮结合于同一类结合位点。我们的结果表明，体外³H-地西泮和³H-氟硝西泮结合位点是体内介导苯二氮䓬各种药理和临床作用的受体。
