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[(±)-12-氯番荔枝碱对脑多巴胺受体的作用]

[Effect of (+/-)12-chloroscoulerine on brain dopamine receptors].

作者信息

Chen L J, Xi Y, Pang D W, Zhou Q T, Jin G Z

机构信息

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.

出版信息

Zhongguo Yao Li Xue Bao. 1996 Mar;17(2):185-9.

PMID:9772676
Abstract

AIM

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 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.

摘要

目的

评估四氢原小檗碱(THPB)和氢化苄基四氢异喹啉(HBTI)对多巴胺(DA)受体的活性。

方法

采用小牛纹状体与D1和D2受体的受体结合试验以及动物行为测试。

结果

(±)12-氯番荔枝碱(CSL)是THPB和HBTI中活性最强的一种。CSL对D1和D2受体的亲和力分别为13和51 nmol.L-1。在大鼠中,CSL对刻板行为表现出拮抗作用并诱发僵住症。然而,在6-羟基多巴胺损伤的大鼠中,CSL对DA受体发挥激动作用。

结论

CSL对DA受体具有双重作用,其作用与(-)千金藤啶碱相似。

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