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新型抗心律失常药物TYB-3823对豚鼠心室肌电生理特性的影响。

Effects of TYB-3823, a new antiarrhythmic drug, on the electrophysiological properties of guinea-pig ventricular muscles.

作者信息

Ohmura T, Nishio M, Kigoshi S, Muramatsu I, Momose Y

机构信息

Department of Pharmacology, Fukui Medical School, Japan.

出版信息

Gen Pharmacol. 1990;21(4):493-7. doi: 10.1016/0306-3623(90)90704-p.

Abstract
  1. The effects of TYB-3823 (B-GYKI 38233), a new antiarrhythmic drug, were electrophysiologically examined in the guinea-pig ventricular muscles. 2. TYB-3823 at concentrations of 1-3 x 10(-7) M significantly prolonged the action potential duration (APD) of the papillary muscle. However, the resting potential, action potential amplitude and maximum rate of depolarization (Vmax) were unaffected by the drug at such concentrations. At a higher concentration (1 x 10(-4) M) TYB-3823 reduced Vmax. 3. Voltage clamp experiments with single ventricular cells revealed that TYB-3823 at concentrations higher than 1 x 10(-7) M reduced the outward potassium currents, especially the time-dependent outward current, but that TYB-3823 failed to affect the calcium current. 4. These results suggested that TYB-3823 at low concentrations reduces the outward potassium current to give rise to a prolongation of APD and that at higher concentrations it additionally inhibits the sodium channels; both the effects may be related to the antiarrhythmic action of this drug.
摘要
  1. 在豚鼠心室肌中对新型抗心律失常药物TYB - 3823(B - GYKI 38233)的作用进行了电生理学研究。2. 浓度为1 - 3×10⁻⁷ M的TYB - 3823显著延长了乳头肌的动作电位时程(APD)。然而,在该浓度下药物对静息电位、动作电位幅度和最大去极化速率(Vmax)没有影响。在较高浓度(1×10⁻⁴ M)时,TYB - 3823降低了Vmax。3. 对单个心室细胞进行的电压钳实验表明,浓度高于1×10⁻⁷ M的TYB - 3823可降低外向钾电流,尤其是时间依赖性外向电流,但TYB - 3823对钙电流没有影响。4. 这些结果表明,低浓度的TYB - 3823通过降低外向钾电流导致APD延长,而在较高浓度时它还会抑制钠通道;这两种作用可能都与该药物的抗心律失常作用有关。

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