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作 者:余雯静[1] 聂辉[1] 袁春华[2] 李享元[1] 李之望[1]
机构地区:[1]华中科技大学同济医学院基础医学院神经生物学系,武汉430030 [2]湖南师范大学生命科学学院,长沙410006
出 处:《华中科技大学学报(医学版)》2008年第2期145-148,共4页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong
基 金:国家自然科学基金资助项目(No.30370456)
摘 要:目的用非洲爪蟾卵母细胞表达之Kv4.2和Kv1.2编码的快和慢钾通道,检验双(7)-他克林对此两种通道是否有抑制作用。方法应用爪蟾卵母细胞注射mRNA进行表达,电压钳记录Kv4.2和Kv1.2钾电流(IK)。结果双(7)-他克林抑制IK(Kv4.2)和IK(Kv1.2)的IC50值分别为(0.23±0.05)μmol/L和(0.24±0.06)μmol/L。结论此种抑制效应可能与在双(7)-他克林作用下表达的Kv4.2和Kv1.2钾通道激活曲线向超极化电压方向偏移有关。Objective To examine whether bis(7) tacrine exerts a similar inhibitory effects on encoding K^+ channels expressed in oocytes of Xenopus laevis as reported previously on rat DRG neurons. Methods Transient and sustained potassium currents were recorded using voltage-clamp techniques on oocytes Xenopus expressing Kv4.2 and Kv1. 2 mRNA. Results It has been identified that bis(7)-tacrine inhibited IK(Kv4.2) and ⅠK(Kv1.2) markedly with IC50 values of (0.23±0.05) μmol/L and (0.24±0.06) μmol/L, respectively. Conclusion The inhibition of bis(7)-tacrine on transient and sustained potassium channels was deduced to be caused by shift of activation curves for these two K^+ channels to the hyperpolarizing direction. These results coincide very well with the phenomenon observed in native KA and KDR channels recorded in rat DRG neurons.
关 键 词:双(7)-他克林 非洲爪蟾卵母细胞 钾通道 抑制效应
分 类 号:R338.8[医药卫生—人体生理学]
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