| 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 |
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| 作者姓名： | Zhong N Fang QZ Zhang Y Qian JQ Zhou ZN |
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| 作者单位： | 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,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,武汉 4130030 中国,上海 200031 |
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| 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(I_(K1))及延迟整流钾通道电流(I_K)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APD_(50)明显缩短;但DDPH(>1μmol·L~(-1))延长APD_(90)。DDPH浓度依赖性地抑制I_K尾电流(I_(K·tail)),EC_(50)为13.3(11.6.6-16.7)μmol·L~(-1)。DDPH(>1.0μmol·L~(-1))明显抑制I_(Kl);同时,DDPH使I_(Kl)翻转电位向正电位方向移动。结论:DDPH对豚鼠心室肌细胞I_(Kl)和I_K具有明显的抑制作用。
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| 关 键 词： | 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 膜片箝技术 心肌 钾通道 动作电位 |
Inhibitory effect of 1-(2, 6-dimethylphenoxy)-2-(3, 4-dimethoxyphenyl-ethylamino) propane hydrochloride on inward rectifier and delayed rectifier K+ currents in guinea pig ventricular myocytes |
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| Zhong N,Fang QZ,Zhang Y,Qian JQ,Zhou ZN.Inhibitory effect of 1-(2, 6-dimethylphenoxy)-2-(3, 4-dimethoxyphenyl-ethylamino) propane hydrochloride on inward rectifier and delayed rectifier K+ currents in guinea pig ventricular myocytes[J].Acta Pharmacologica Sinica,2000,21(4):301-305. |
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| Authors: | Zhong N Fang Q Z Zhang Y Qian J Q Zhou Z N |
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| Institution: | Shanghai Institute of Physiology, Chinese Academy of Sciences, Shanghai 200031, China. nolannz@sunm.shcnc.ac.cn |
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| Abstract: | AIM: To study the effects of 1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenyl-ethylamino) propane hydrochloride (DDPH) on action potential (AP), inward rectifier K+ current (IK1), and delayed rectifier K+ current (IK) in isolated guinea pig ventricular myocytes. METHODS: Whole cell patch-clamp recording techniques. RESULTS: DDPH 0.1-100 mumol.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 mumol.L-1. However, 90% duration of action potential (APD90) was increased by DDPH (> 1 mumol.L-1). At high concentration (> 10 mumol.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 mumol.L-1 and 78% at 100 mumol.L-1. EC50 for DDPH inhibiting IK was 13.3 (11.6-16.7) mumol.L-1. DDPH also blocked IK1. DDPH at high concentration (> 10 mumol.L-1) shifted the reverse potential of IK1 positively. All the effects of DDPH were reversible after washout. CONCLUSION: DDPH blocked both IK1 and IK current in guinea pig ventricular myocytes. |
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| Keywords: | 1-( 2 6-dimethylphenoxy )-2-( 3 4-dimethoxyphenyl-ethylamino ) propane hydrochloride patch-clamp techniques myocardium potassium chan-nels action potentials |
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