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1-(2,6-二甲基苯氧基)-2-(3,4-二甲氧基苯乙氨基)丙烷盐酸盐抑制豚鼠心室肌细胞内向整流和延迟整流钾电流(英文)

Inhibitory effect of l-( 2, 6-dimethylphenoxy )-2-( 3, 4-dimethoxy- phenyl-ethylamino) propane hydrochloride on inward rectifier and delayed rectifier K+ currents in guinea pig ventricular myocytes

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【作者】 钟宁方奇志张翼钱家庆周兆年

【Author】 ZHONG Ning, FANG Qi-Zhi, ZHANG Yi, QIAN Jia-Qing, ZHOU Zhao-Nian (1Shanghai Institute of Physiology, Chinese Academy of Sciences, Shanghai 200031; 2Department of Pharmacology, Tongji Medical University, Wuhan 430030, China)

【机构】 中国科学院上海生理研究所同济医科大学药理教研室中国科学院上海生理研究所 上海 200031武汉 4130030 中国上海 200031上海 200031

【摘要】 目的:研究1-(2,6-二甲基苯氧基)-2-(3,4-二甲氧基苯乙氨基)丙烷盐酸盐(DDPH)对心室肌细胞动作电位(AP)、内向整流钾通道电流(IK1)及延迟整流钾通道电流(IK)的影响。方法:全细胞膜片箝技术。结果:DDPH 10,100μmol·L-1使豚鼠心室肌细胞AP时程APD50明显缩短;但DDPH(>1μmol·L-1)延长APD90。DDPH浓度依赖性地抑制IK尾电流(IK·tail),EC50为13.3(11.6.6-16.7)μmol·L-1。DDPH(>1.0μmol·L-1)明显抑制IKl;同时,DDPH使IKl翻转电位向正电位方向移动。结论:DDPH对豚鼠心室肌细胞IKl和IK具有明显的抑制作用。

【Abstract】 AIM: To study the effects of 1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenyl-ethylamino) propane hydrochlo-ride (DDPH) on action potential (AP), inward rectifier K+ current (IKl), and delayed rectifier K+ current (IK) in isolated guinea pig ventricular myocytes. METHODS: Whole cell patch-clamp recording techniques. RESULTS: DDPH 0.1 - 100 μumol · L-1 decreased 50 % duration of action potential (APD50) concentration-dependently. APD50 was shortened from (493 ± 58) to (262 ±38) ms (n = 7 cells from 5 guinea pigs, P < 0.01) by DDPH 10 μmol· L -1. However, 90 % duration of action potential (APD90) was increased by DDPH ( > 1 μmol · L-1). At high concentration ( > 10 μmol · L-1) DDPH decreased resting membrane potential (RP) and amplitude of action potential (APA). DDPH inhibited tail current of IK(IK·tail) concentration-dependently, 46 % at 10 μmol · L-1 and 78 % at 100 μmol · L-1. EC50 for DDPH inhibiting IK was 13.3 (11.6 - 16.7) μmol·L-1. DDPH also blocked IKl. DDPH at high concentration ( > 10 μmol·L-1) shifted the reverse potential of IKl positively. All the effects of DDPH were reversible after washout. CONCLUSION: DDPH blocked both IKl and IK current in guinea pig ventricular myocytes.

  • 【文献出处】 Acta Pharmacologica Sinica ,中国药理学报(英文版) , 编辑部邮箱 ,2000年04期
  • 【分类号】R96
  • 【被引频次】1
  • 【下载频次】15
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