I－G－018动物体内受体结合研究

• 作 者: 匡安仁 谭天秩 钟裕国
• 出 处: 华西医科大学学报
• 发表日期: 1994年02期
• 关键词: 苯二氮受体 受体结合 生理条件 抑制率 竞争性抑制 延脑 二丁基 大鼠 特异性 静脉注射给药

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。

In vivo competitive inhibition experiments in mice and rats demonstrated that diazepam and α-dibutyl-p-hydroxybenzyl alcohol (G-018) inhibited both 125 I-G-018 and brain benzene Nitrogen receptor specific binding. Inhibition rate in the cerebral cortex, cerebellum, hippocampus and midbrain higher, no significant inhibition of the brain and hypothalamus, the level of inhibition and benzodiazepine receptors in the brain distribution consistent with animal experiments and in vitro receptor analysis Consistent with the results, demonstrating the specific binding of G-018 to the benzodiazepine receptor under in vivo physiological conditions.