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Inhibition of transmembrane K+ currents in mammalian ventricular myocytes by antiarrhythmic agent RP62719
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- Author:
- No author available
- Journal Title:
- ACTA PHYSIOLOGICA SINICA
- Issue:
- 5
- DOI:
- 10.3321/j.issn:0371-0874.2000.05.015
- Key Word:
- RP62719;内向整流钾电流;瞬时外向钾电流;延迟外向钾电流;半数抑制浓度(IC50)
Abstract： 使用全细胞膜片箝技术, 研究RP62719对内向整流钾电流(IK1)、瞬时外向钾电流(Ito)和延迟外向整流钾电流(IK)的作用, 并探讨其抗心律失常作用的机制.实验结果表明, 在指令电压为-100 mV时, RP62719可显著抑制豚鼠心室肌细胞IK1, 半数抑制浓度(IC50)为5.0±1.0 μmol/L.RP62719 10 μmol/L在+40 mV时对犬心室肌细胞Ito抑制率为84.0±4.4%, IC50为1.2±0.51 μmol/L.在+40 mV时, 50 μmol/L RP62719还可使豚鼠心室肌细胞IKstep 减少50.0±8.3%, IKtail减少56.0±4.9%, IC50分别为4.2±0.8 μmol/L和3.3±0.75 μmol/L.提示RP62719抗心律失常的离子机制与其对IK1、Ito及IK的抑制有关.
- [1]J G, McLarnon,R, Xu.Actions of the benzopyran compound terikalant on macroscopic currents in rat ventricular myocytes.[J].1995,275(1).