氯代斯阔任对多巴胺受体的作用  

Effect of ( ± ) 12-chloroscoulerine on brain dopa- mine receptors

作　　者：陈丽娟[1] 奚勇 庞大伟 周启霆 金国章 

机构地区：[1]中国科学院上海药物研究所

出　　处：《中国药理学报》1996年第2期185-189,共5页Acta Pharmacologica Sinica

基　　金：Supported by the National Natural Science Foundation of China;№ 39130091;the State Key Laboratory of Drug Research;Shanghai Institute of Materia Medica;Chinese Academy of Sciences;№ K016.

摘　　要：目的: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D_1和D_2受体进行放射受体结合分析并进行大鼠行为实验。结果:(±)12-氯代斯阔任(CSL)对D_1和D_2受体的亲和力分别为13和51nmol·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。AIM: To assess potencies of tetrahy-droprotoberberines ( THPB ) and hydrobenzyl-tetrahydroisoquinolines (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 to D1 and D2 receptors were 13 and 51 nmol·L-1, 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.

关 键 词：氯代斯阔任 多巴胺受体 受体 

分 类 号：R971[医药卫生—药品] R966[医药卫生—药学]