张广钦, 郝雪梅, 马玉萍, 周培爱, 吴才宏, 戴德哉. 苄普地尔对豚鼠甲亢性肥厚心肌中延迟整流钾电流的抑制作用J. 药学学报, 2001, 36(7): 489-492.
引用本文: 张广钦, 郝雪梅, 马玉萍, 周培爱, 吴才宏, 戴德哉. 苄普地尔对豚鼠甲亢性肥厚心肌中延迟整流钾电流的抑制作用J. 药学学报, 2001, 36(7): 489-492.
ZHANG Guang-qin, HAO Xue-mei, MA Yu-ping, ZHOU Pei-ai, WU Cai-hong, DAI De-zai. BEPRIDIL INHIBITION ON THE DELAYED RECTIFIER K+ CURRENTS IN THYROXINE INDUCED HYPERTROPHIED GUINEA PIG VENTRICULAR MYOCYTESJ. Acta Pharmaceutica Sinica, 2001, 36(7): 489-492.
Citation: ZHANG Guang-qin, HAO Xue-mei, MA Yu-ping, ZHOU Pei-ai, WU Cai-hong, DAI De-zai. BEPRIDIL INHIBITION ON THE DELAYED RECTIFIER K+ CURRENTS IN THYROXINE INDUCED HYPERTROPHIED GUINEA PIG VENTRICULAR MYOCYTESJ. Acta Pharmaceutica Sinica, 2001, 36(7): 489-492.

苄普地尔对豚鼠甲亢性肥厚心肌中延迟整流钾电流的抑制作用

BEPRIDIL INHIBITION ON THE DELAYED RECTIFIER K+ CURRENTS IN THYROXINE INDUCED HYPERTROPHIED GUINEA PIG VENTRICULAR MYOCYTES

  • 摘要: 目的 研究苄普地尔(bepridil)对肥厚心肌细胞延迟整流钾电流(IK)中快激活成份(IKr)和慢激活成份(IKs)及内向整流钾电流(IK1)的作用。方法 全细胞膜片钳技术。结果 在肥厚心肌细胞中,Bepridil 30 μmol·L- 1 对IKrIKs有阻断作用,抑制率分别为20.9% (0 mV)和27.2 % (+50 mV)。“Envelopeoftail”显示bepridil对IKs的阻断作用大于IKr。Bepridil(1 - 100 μmol·L-1 )浓度依赖性的阻断IKsIKr,其IC50 分别为23.8μmol·L-1 和46.7μmol·L-1 。Bepridil 30 μmol·L-1 也能阻断IK1 ,抑制率为15.1% (- 100 mV) ,但不影响其反转电位。结论 Bepridil对甲亢性豚鼠肥厚心肌中IKs,IKrIK1有阻断作用

     

    Abstract: AIM To study the effects of bepridil on the rapidly activating component (IKr), the slowly activating component (IKs) of the delayed rectifier potassium current and the inward rectifier potassium current (IK1) in hypertrophied guinea pig ventricular myocytes. METHODS The whole cell patch clamp techniques were used. RESULTS In hypertrophied guinea pig ventricular myocytes, bepridil 30 μmol·L-1 markedly inhibited IKr and IKs (by 20.9% and 27.2% at 0 mV and +50 mV, respectively). The effect of bepridil on IKs was larger than on IKr. Bepridil 30 μmol·L-1 also significantly inhibited the inward component of IK1(by 15.1% at +100 mV), but the reverse potential of IK1 was unaffected. Bepridil (1-100 μmol·L-1 ) was shown to inhibit IKr and IKs in a concentration-dependent manner. Their IC50 were 46.7 μmol·L-1 and 23.8 μmol·L-1, respectively. CONCLUSION Bepridil inhibit IKr, IKs and IK1 in hypertrophied guinea pig ventricular myocytes, which may be important in understanding the antiarrhythmic effects of this drug.

     

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