氯代斯阔任对多巴胺受体的作用

摘要

比较四氢原小檗碱同类物(THPB)和氢化苄基-四氢异喹啉类(HBTI)两类化合物对DA受体的作用强度,从而找出对DA受体作用更有效的化合物.方法:用小牛纹状体膜蛋白对D1和D2受体进行放射受体结合分析并进行大鼠行为恃?结果:(±)12-氯代斯阔任(CSL)对D1和D2受体的亲和力分别为13和51 nmol·L-1,与先导化合物左旋千金藤立定[(-)stepholidine,SPD]在同一水平,动物行为实验表明它对DA受体有阻滞作用,但在超敏条件下,出现激动作用,这些特点与SPD的作用类似.结论:CSL是目前THPB中对DA受体作用最强者,与SPD类似是对DA受体阻滞剂兼有激动作用.%To assess potencies of tetrahydroprotoberberines ( THPB ) and hydrobenzyltetrahydroisoquinolines (HBTI) on DA receptors.METHODS: The receptor binding assay with calf striatum to D1 and D2 receptors, and the animal behavior tests were used. RESULTS: ( ± ) 12-Chloroscoulerine (CSL) was the most potent one among the THPB and HBTI. The affinities of CSL respectively. In rats, CSL showed an antagonistic effect on the stereotypy and induced catalepsy. In the 6-OHDA lesioned rats, however, CSL exerted the agonistic effect to DA receptors. CONCLUSION: CSL had dual actions to DA receptors and its effects were similar to that of ( - )stepholidine.