左旋千金藤立定拮抗D_2受体激动剂对大鼠突触体酪氨酸羟化酶活性的负反馈调节(英文)  

(-)-Stepholidine antagonizes the inhibition by D_2 receptor agonists on synaptosomal tyrosine hydroylase in rat corpus striatum

作　　者：胡刚 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》1995年第4期376-379,共4页Acta Pharmacologica Sinica

基　　金：Supported by the National Natural Science Foundation of China (№39130091);the Key Laboratory for Drug Research, Shanghai Institute of Materia Mediea (K-016).

摘　　要：目的:研究左旋千金藤立定(SPD)对大鼠纹状体突触体酪氨酸羟化酶(TH)活性的影响.方法:利用高效液相-电化学法(HPLC-ECD)检测ι-DOPA的含量变化.结果:选择性D_2受体激动剂N-0437和喹吡罗均能抑制大鼠纹状体TH的活性,D_1受体激动剂SKF 38393和SPD都不能抑制TH的活性;D_2受体阻滞剂螺哌隆和SPD均能拮抗D_2受体激动剂对TH的抑制作用.结论:D_2受体介导突触前DA受体的负反馈调控,SPD对D_2受体无激动作用,而是D_2受体的阻滞剂.To evaluate the action of (-)-stepholi-dine (SPD), a novel dopamine (DA) receptor antagonist, on inhibition by presynaptic D2 receptor agonists on the activity of synaptosomal tyrosine hydroxylase (TH) in the striatum. METHOD:The TH activity was measured by HPLC-ECD. RESULTS: The mixed DA receptor agonist apomorphine (Apo 10. 4 nmol L-1) and selective D2 receptor agonists N-0437 (0.4 pmol L-1 ) and quinpirole (0.8 umol L-1) inhibited the activity of TH, while selective D1 receptor agonist SKF 38393 (0.001 -10μmol L-1) and SPD (1-100μmol L-1) failed to inhibit the TH actively. The inhibition of N-0437 and quinpirole were antagonized by D2 receptor antagonist spiperone and SPD. CONCLUSION : The negative feedback regulation of presynaptic DA receptors is mediated via D2 receptors and SPD is an antagonist on presynaptic D2 DA receptors.

关 键 词：小檗因类 左旋千金藤立定 反馈调节 突触体 

分 类 号：R965.2[医药卫生—药理学]