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新型抗心律失常药物EGIS-7229对离体豚鼠乳头肌的电生理效应

Electrophysiological effects of EGIS-7229, a new antiarrhythmic agent, in isolated guinea pig papillary muscle.

作者信息

Pankucsi C, Bányász T, Magyar J, Gyönös I, Kovács A, Szénási G, Varró A, Nánási P P

机构信息

Department of Physiology, University Medical School of Debrecen, Hungary.

出版信息

Gen Pharmacol. 1997 Aug;29(2):275-80. doi: 10.1016/s0306-3623(96)00461-2.

Abstract
  1. The cellular electrphysiological effects of EGIS-7229, a novel antiarrhythmic agent, were studied in guinea pig papillary muscles with the use of conventional microelectrode techniques. 2. The drug had a concentration-dependent biphasic effect on action potential duration (APD). APD was significantly lengthened at low concentration (3 mumol/1), whereas it was shortened at concentrations higher than 10 mumol/l. 3. At concentrations higher than 10 mumol/l, the drug decreased the maximum velocity of action potential upstroke (Vmax), the force contraction, and altered the restitution kinetics of APD. 4. The effect of EGIS-7229 on Vmax was frequently dependent; it was most prominent at short pacing cycle lengths (use-dependent block). 5. On the basis of present results, EGIS-7229 appears to carry mixed class I and class III characteristics. Class III properties are present at low concentrations, whereas, at higher concentrations, class I actions may be predominant.
摘要
  1. 采用传统微电极技术,在豚鼠乳头肌中研究了新型抗心律失常药物EGIS - 7229的细胞电生理效应。2. 该药物对动作电位时程(APD)具有浓度依赖性双相效应。低浓度(3 μmol/L)时APD显著延长,而浓度高于10 μmol/L时则缩短。3. 浓度高于10 μmol/L时,该药物降低动作电位上升的最大速度(Vmax)、收缩力,并改变APD的恢复动力学。4. EGIS - 7229对Vmax的影响通常具有频率依赖性;在短起搏周期长度时最为显著(频率依赖性阻滞)。5. 根据目前的结果,EGIS - 7229似乎具有I类和III类的混合特性。低浓度时呈现III类特性,而在较高浓度时,I类作用可能占主导。

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