甲苯喹哌对培养爪蟾胚胎肌细胞和神经细胞离子通道的作用(英文)  

Effects of toquipidine on ionic channels of cultured embryonic Xenopus laevis myoblasts and neurons

作　　者：郑平[1] 陈功[2] 史念慈[1] 周思平[1] 鲁映青[1] 姚明辉[1] 何曾佑 

机构地区：[1]上海医科大学基础医学院药理教研室,上海200032 [2]中国科学院上海生理研究所,上海200031 [3]扬州制药厂

出　　处：《中国药理学报》1995年第5期427-439,共13页Acta Pharmacologica Sinica

摘　　要：目的:研究新型抗心律失常药甲苯喹哌对离子通道的作用.方法:通过膜片钳技术记录培养爪蟾胚胎肌细胞和神经细胞全细胞离子通道电流.结果:甲苯喹哌(0.1,1,10,100μmolL^(-1))可浓度依赖性地抑制肌细胞的钠通道,其IC_(50)为7.2μmol L^(-1)(5.3—9.8μmol L^(-1)).甲苯喹哌(10μmol L^(-1))可抑制神经细胞的高电压激活的钙通道.然而,肌细胞上的稳态外向钾电流却受到甲苯喹哌(10μmol L^(-1))的激活.结论:甲苯喹哌抑制钠、钙通道,但激活稳态外向钾通道.AIM:To study the effects of toquipidine (1~p-methy 1-phenyl- 2- ( a-piperidinoacetyl) -1, 2,3,4-tetrahydroisoquinoline hydrochloride, Toq), a new anti-arrhythmic agent first synthesized in China, on ionic channels. METHODS: Ionic channel currents were recorded by whole-cell patch clamp technique in culturedembryonic Xenopus laevis myoblasts and neurons. RESULTS:Toq (0.1,1, 10, and 100μmol L-1) caused a concentration-dependent inhibition of the Na+ currents with IC50 7.2μmol L-1(5.3 -9.8μmol L-1). Toq (10μmol L-1) also suppressed the high-voltage-activated Ca2+ currents in neurons. But the steady-state outward K+ currents in myoblasts were activated by Toq (10μmol L-1). CONCLUSION:Toq blocked the Na+ and Ca2+ channels and opened the steady-state outward K+ channels.

关 键 词：甲苯喹哌 电生理学 神经元 钠通道 钙通道 

分 类 号：R965.2[医药卫生—药理学]