| (1R,2R) -SIPI5358和SIPI5358对未分化PC12细胞延迟整流钾电流的抑制作用 |
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| 引用本文： | 周慧,汪溪洁,翁志洁,马璟,李建其.(1R,2R) -SIPI5358和SIPI5358对未分化PC12细胞延迟整流钾电流的抑制作用[J].中国医药工业杂志,2012,43(6):443-447. |
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| 作者姓名： | 周慧 汪溪洁 翁志洁 马璟 李建其 |
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| 作者单位： | 1. 中国医药工业研究总院上海医药工业研究院,国家上海新药安全评价研究中心,上海201203
2. 中国医药工业研究总院上海医药工业研究院,上海,200040 |
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| 基金项目： | 国家“十二五”重大新药创制科技重大专项(2012ZX09102-101-008) |
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| 摘 要： | 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)μmol/L.l μmol/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 μmol/L的SIP15358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SIP15358对Ⅰx的影响可能与其神经毒性有关.
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| 关 键 词： | (1R 2R)-SIPI5358 SIPI5358 未分化PC12细胞 延迟整流钾电流 全细胞膜片钳 |
Inhibition of(1R,2R)-SIPI5358 and SIPI5358 on Delayed Rectifier Potassium Current in Undifferentiated PC12 Cells |
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| Authors: | ZHOU Hui WANG Xijie WENG Zhijie MA Jing LI Jianqi |
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| Institution: | 1.National Shanghai Center for New Drug Safety Evaluation & Research,Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry,Shanghai 201203;2.Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry,Shanghai 200040) |
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| Abstract: | The effects of(1R,2R)-SIPI5358 and SIPI5358 on the delayed rectifier potassium current(IK) in undifferentiated PC12 cells were recorded with whole-cell patch clamp technique.The results showed that the two compounds had a concentration-and voltage-dependent inhibition on IK.The IC50 values of(1R,2R)-SIPI5358 and SIPI5358 were(0.64±0.17) and(12.05±3.31)μmol/L,respectively.The(1R,2R)-SIPI5358 at the concentration of 1 μmol/L shifted the IK steady-state activation and inactivation curves in the hyperpolarizing direction by 4 and 20 mV.The SIPI5358 at the concentration of 20 μmol/L shifted the IK steady-state activation curve in the depolarizing direction by 7 mV and shifted the inactivation curve in the hyperpolarizing direction by 21 mV.The effects of(1R,2R)-SIPI5358 and SIPI5358 on IK might be related to their neurotoxicity. |
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| Keywords: | (1R 2R)-SIPI5358 SIPI5358 undifferentiated PC12 cells delayed rectifier potassium current whole-cell patch clamp |
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