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.
出处
《中国药理学报》
CSCD
1995年第5期427-439,共13页
Acta Pharmacologica Sinica
关键词
甲苯喹哌
电生理学
神经元
钠通道
钙通道
toquipidine
isoquinolines
electrophysiology
cultured cells
muscles
neurons
sodium channels
calcium channels
potassium channels
Xenopus laevis