Chen L J, Xi Y, Pang D W, Zhou Q T, Jin G Z
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhongguo Yao Li Xue Bao. 1996 Mar;17(2):185-9.
To assess potencies of tetrahydroprotoberberines (THPB) and hydrobenzyltetrahydroisoquinolines (HBTI) on DA receptors.
The receptor binding assay with calf striatum to D1 and D2 receptors, and the animal behavior tests were used.
(+/-) 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.
CSL had dual actions to DA receptors and its effects were similar to that of (-)stepholidine.
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。
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。
(±)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。
CSL对DA受体具有双重作用,其作用与(-)千金藤啶碱相似。