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

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Author:
No author available
Journal Title:
ACTA PHARMACEUTICA SINICA
Issue:
7
DOI:
10.3321/j.issn:0513-4870.2001.07.003
Key Word:
苄普地尔;甲状腺素;肥厚心肌细胞;钾通道;膜片钳技术

Abstract: 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(I Kr)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IKr及IKs 有阻断作用,抑制率分别为20.9%(0 mV)和27.2%(+50 mV)."Envelope of tail”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IKs及IKr,其IC50分别为23.8 μmol*L-1和46.7 μmol*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,IKr及IK1有阻断作用.

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