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Inhibitory effects of vinpocetine on sodium current in rat cardiomyocytes

Inhibitory effects of vinpocetine on sodium current in rat cardiomyocytes

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【作者】 魏苑史念慈钟慈声郑平梁子钧

【Author】 WEI Yuan, SHI Nian Ci 2 , ZHONG Ci Sheng, ZHENG Ping 3 , LIANG Zi Jun 4 ( Department of Biophysics, 2 Department of Pharmacology, 3 Department of Neurobiology, School of Basic Medical Sciences, Shanghai Medical University, Shangh

【机构】 上海医科大学基础医学院生物物理教研室

【摘要】 目的:研究长春西汀对心肌细胞钠电流的作用.方法:用全细胞膜片箝技术记录大鼠心肌细胞钠电流.结果:长春西汀可逆性抑制心肌细胞钠电流的作用为剂量依赖性和电压依赖性,但未发现频率或使用依赖性.长春西汀10-80μmol·L-1,对钠电流的抑制作用为13%±2%至75%±6%.半数抑制浓度IC50值(95%可信限)为364(281-471)μmol·L-1.在膜电位以10mV的间隔从-90mV阶梯状去极化至+40mV时,抑制作用呈逐渐增加的趋势,约在0mV左右达到最大抑制.长春西汀对钠通道的稳态激活和失活过程的影响,可使钠窗电流(缓慢失活的钠电流)减少.结论:长春西汀抑制大鼠心肌细胞的钠电流

【Abstract】 AIM: To study the effects of vinpocetine (Vin) on the sodium current ( I Na ) in cardiomyocytes. METHODS: The sodium current in adult rat ventricular myocytes was measured by whole cell patch clamp technique. RESULTS: The I Na in cardiomyocytes was blocked reversibly by Vin, in concentration dependent and voltage dependent manner, but not rate or use dependent. The I Na was attenuated by 13 %-75 % when the Vin concentration was raised from 10 to 80 μmol·L -1 . The IC 50 (95 % confidence limits) was 36.4 (28 1-47 1) μmol·L -1 . When the membrane potential depolarized over the range of -90 mV to +40 mV in 10 mV step, inhibitory effect of Vin on the I Na was 39 % at first, then maintained at a higher level, about 52 %±5 %. The maximal depression ( 57 % ) reached at about 0 mV. Vin influenced both the activation and inactivation processes of sodium channel, and resulted in attenuation of the window currents (the slowly inactivating sodium currents). CONCLUSION: Vin inhibited sodium currents in rat ventricular myocytes.

  • 【文献出处】 Acta Pharmacologica Sinica ,中国药理学报(英文版) , 编辑部邮箱 ,1997年05期
  • 【分类号】R966
  • 【被引频次】4
  • 【下载频次】9
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