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利用全细胞膜片钳技术研究新化合物(1R,2R)-SIPI5358和SIPI5358对未分化PC12细胞延迟整流钾电流(IK)的影响。结果表明,(1R,2R)-SIPI5358和SIPI5358可抑制未分化PC12细胞的IK,且抑制作用具有浓度和电压依赖性,IC50分别为(0.64±0.17)和(12.05±3.31)mol/L。1 mol/L的(1R,2R)-SIPI5358可使未分化PC12细胞的IK稳态激活曲线和失活曲线向超极化方向移动4和20 mV。20 mol/L的SIPI5358可使未分化PC12细胞的IK稳态激活曲线向去极化方向移动7mV;使失活曲线向超极化方向移动21 mV。(1R,2R)-SIPI5358和SIPI5358对IK的影响可能与其神经毒性有关。
The effects of novel compounds (1R, 2R) -SIPI5358 and SIPI5358 on delayed rectifier potassium current (IK) in undifferentiated PC12 cells were investigated using whole-cell patch clamp technique. The results showed that (1R, 2R) -SIPI5358 and SIPI5358 inhibited IK in undifferentiated PC12 cells in a concentration-and voltage-dependent manner with IC50 of (0.64 ± 0.17) and (12.05 ± 3.31) mol / L, respectively. 1 mol / L of (1R, 2R) -SIPI5358 shifted the IK steady-state activation and inactivation curves of undifferentiated PC12 cells to hyperpolarizations by 4 and 20 mV. 20 mol / L of SIPI5358 can promote IK steady-state activation curve of undifferentiated PC12 cells to 7mV in depolarization direction and 21μV of inactivation curve to hyperpolarization. The effects of (1R, 2R) -SIPI5358 and SIPI5358 on IK may be related to their neurotoxicity.