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苄普地尔抑制大鼠海马CA1区锥体细胞钠电流(英文)

Bepridil inhibition of sodium current in rat hippocampal CA1 neurons

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【作者】 胡慧娟阳冬梅戴德哉吴才宏周培爱

【Author】 HU Hui-Juan, YANG Dong-Mei, DAI De-Zai, WU Cai-Hong, ZHOU Pei-Ai(Department of Pharmacology of Chinese Materia Medica, Research Division of Pharmacology,China Pharmaceutical University, Nanjing 210009, China;National Laboratory of Biomembrane and Membrane Biotechnology, Peking University, Beijing 100871, China)

【机构】 中国药科大学中药药理教研室北京大学生物膜与膜生物工程国家重点实验室中国药科大学药理研究室北京大学生物膜与膜生物工程国家重点实验室 南京 210009北京 中国 100871南京 210009北京 中国 100871

【摘要】 目的:研究苄普地尔对大鼠海马CA1区锥体细胞钠电流的影响。方法:膜片箝全细胞记录技术。结果:苄普地尔显著降低大鼠海马CA1区锥体细胞钠电流,作用呈时间及浓度依赖关系。苄普地尔10μmol·L-1的半阻断时间约为10min。IC50为2.6(2.3-2.9)μmol·L-1。苄普地尔10μmol·L-1右移最大电流的激活电位10mV,左移半失活膜电位18mV,表明其电压依赖地影响钠通道的激活和失活过程。结论:苄普地尔阻断大鼠海马CA1区锥体细胞钠电流,可能是其抗脑缺血机制之一。

【Abstract】 AIM: To study the effects of bepridil on sodium current in rat hippocampal neurons. METHODS: All experiments were performed on acutely isolated hippocampal pyramidal neurons by means of whole-cell patch-clamp techniques. Recording media contained ion channel blockers to allow the selective activation of voltage-dependent sodium currents. RESULTS: Bepridil reduced the amplitudes of sodium current in time- and concentration-dependent manners. The half-blocking time was about 10 min in bepridil 10 μmol·L-1, and IC50, was 2.6 (2.3 - 2.9) μmol·L-1. Bepridil 10 μmol·L-1 shifted the maximal activation of sodium current from - 50 mV to - 40 mV, and the characteristic voltage of inactivation from - 71 mV to -89mV without changing the slope factor. CONCLUSION: Bepridil blocked voltage-dependent sodium current of hippocampal CA1 neurons and might have therapeutic actions for ischemia-induced brain damage.

【基金】 Project supported by the National Natural Science Foundation of China, № 39890883.
  • 【文献出处】 Acta Pharmacologica Sinica ,中国药理学报(英文版) , 编辑部邮箱 ,1999年09期
  • 【分类号】R96
  • 【被引频次】2
  • 【下载频次】3
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