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.