I－G－018动物体内受体结合研究

￣(125)I-α-sec-butyl-p-hydroxybenzyl alcohol Receptor Competetive Binding Assays in Animal Body

通过小鼠和大鼠的体内竞争性抑制实验，证明了安定和α－第二丁基对羟基苄醇（Ｇ－０１８）在动物体内均能抑制￣（１２５）Ｉ－Ｇ－０１８与脑苯二氮受体的特异性结合。抑制率以大脑皮层、小脑、海马和中脑较高，延脑和下丘脑无明显抑制作用，抑制率的高低与苯二氮受体在脑内的分布一致，动物体内实验与体外受体分析的结果一致，从而在体内生理条件下证明了Ｇ－０１８与脑苯二氮受体的特异性结合。

Based on the receptor competetivebinding assays in the mice and rat body,it has beenproved that both diazepam and α-sec-butyl-p-hydroxy-benzyl alcohol(G-018)can inhibit ￣(125)I-G-018 bindingwith brain benzodiazepine receptor.Inhibiting effectswere obvious in the cortex, cerebellum,hippocampusand midbrain,But in the medullao blongata and hy-pothalamus no inhibiting effect was observed.Experi-mental results have demonstrated that the inhibitingeffect is consistent with distribution of benzodiazepinereceptor in the brain. Also,experimental results haveshown no difference between in vitro and in vivo. TheG-018 binding with benzodiazepine receptor has beenclarified under phvsiologic conditions.