12-氯番荔枝碱对映体对动物行为与多巴胺受体作用的比较。
Comparison of 12-chloroscoulerine enantiomers on animal behavior to dopamine receptors.
作者信息
Chen L J, Zhou Q T, Dong Z J, Yu L P, Jin G Z
机构信息
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 200031, China.
出版信息
Zhongguo Yao Li Xue Bao. 1999 Oct;20(10):884-8.
AIM
To compare the pharmacological characteristics of 12-chloroscoulerine (CSL) enantiomers to dopamine (DA) receptors.
METHODS
Radioligand receptor binding assay with calf striatum and behavioral tests of mice or rats were used.
RESULTS
In the competitive binding assay, the affinities (Ki) of l-CSL to D1 and D2 receptors were 5.7 nmol.L-1, while those of d-CSL for D1 and D2 receptors were 135 and 9150 nmol.L-1, respectively. The Ki of dl-CSL to D1 and D2 receptors were 8.9 and 9.6 nmol.L-1, respectively, which were slightly weaker than that of l-CSL. In the behavioral experiments, CSL enantiomers 5-60 mg.kg-1 antagonized the stereotypy induced by apomorphine in rats, and 5-150 mg.kg-1 produced catalepsy. The enantiomers 10-60 mg.kg-1 reduced the mice jumping behavior induced by amphetamine + levodopa. l-CSL 10-80 mg.kg-1 antagonized the spontaneous locomotor activity of normal or amphetamine-treated mice.
CONCLUSION
CSL enantiomers are antagonists to DA receptors: l-CSL > dl-CSL >> d-CSL.
目的
比较12-氯番荔枝碱（CSL）对映体与多巴胺（DA）受体的药理学特性。
方法
采用小牛纹状体放射性配体受体结合试验及小鼠或大鼠行为学试验。
结果
在竞争性结合试验中，l-CSL对D1和D2受体的亲和力（Ki）分别为5.7 nmol·L-1，而d-CSL对D1和D2受体的亲和力分别为135和9150 nmol·L-1。dl-CSL对D1和D2受体的Ki分别为8.9和9.6 nmol·L-1，略弱于l-CSL。在行为学实验中，CSL对映体5-60 mg·kg-1可拮抗阿扑吗啡诱导的大鼠刻板行为，5-150 mg·kg-1可产生僵住症。对映体10-60 mg·kg-1可减少苯丙胺+左旋多巴诱导的小鼠跳跃行为。l-CSL 10-80 mg·kg-1可拮抗正常或苯丙胺处理小鼠的自发运动活性。
结论
CSL对映体是DA受体拮抗剂：l-CSL > dl-CSL >> d-CSL。
Zotero 插件