范礼理, 宋珍, 王天佑. 羟苯氨酮对豚鼠心肌细胞膜Na+和Ca2+ 离子通道的影响羟苯氨酮对豚鼠心肌细胞膜Na+和Ca2+ 离子通道的影响J. 药学学报, 2004, 39(6): 410-414.
引用本文: 范礼理, 宋珍, 王天佑. 羟苯氨酮对豚鼠心肌细胞膜Na+和Ca2+ 离子通道的影响羟苯氨酮对豚鼠心肌细胞膜Na+和Ca2+ 离子通道的影响J. 药学学报, 2004, 39(6): 410-414.
FAN Li-li, SONG Zhen, WANG Tian-you. Effect of oxyphenamone on sodium and calcium channels of guinea pig myocardial cellsJ. Acta Pharmaceutica Sinica, 2004, 39(6): 410-414.
Citation: FAN Li-li, SONG Zhen, WANG Tian-you. Effect of oxyphenamone on sodium and calcium channels of guinea pig myocardial cellsJ. Acta Pharmaceutica Sinica, 2004, 39(6): 410-414.

羟苯氨酮对豚鼠心肌细胞膜Na+和Ca2+ 离子通道的影响羟苯氨酮对豚鼠心肌细胞膜Na+和Ca2+ 离子通道的影响

Effect of oxyphenamone on sodium and calcium channels of guinea pig myocardial cells

  • 摘要: 目的探讨羟苯氨酮(oxyphenamone)的正性肌力作用机制。方法用膜片钳全细胞记录技术测定心肌细胞膜Na+ 电流与L型Ca2+电流。结果羟苯氨酮剂量依赖性地明显抑制豚鼠心肌细胞膜Na+ 电流,促进Na+ 通道失活,并延长其恢复时间;它对Ca2+电流的影响呈双向性,2~10 μmol·L-1 使电流增加,促进钙通道的激活过程;20与50 μmol·L-1时则使Ca2+电流明显抑制。结论羟苯氨酮的正性肌力作用不是通过激活钠通道,也不完全依赖于激活L型钙通道,它对钠通道的抑制和在高浓度时对L型钙通道的抑制提示该药可能具有抗心律失常作用。

     

    Abstract: AimTo investigate the mechanism of the positive inotropic effect of oxyphenamone. MethodsWith the patch clamp technique and whole cell recording, the sodium and L type calcium currents of myocytes isolated from ventricular myocardium of adult guinea pigs were studied. Results5-50 μmol·L-1oxyphenamone not only significantly inhibited Na+ current, but also promoted the process of inactivation and prolonged the recovery time of the inactivation. The action of oxyphenamone on L type calcium channel was dual. The inward calcium current was increased with 2-10 μmol·L-1oxyphenamone but decreased when the concentration of the drug was elevated to 20-50 μmol·L-1 . ConclusionThe mechanism of the positive inotropic effect of oxyphenamone is neither due to the activation of sodium channel nor entirely depending upon the activation of L type calcium channel. The effects of inhibiting sodium current and, at a high concentration, blocking L type calcium current suggest that oxyphenamone may have an antiarrhythemia action.

     

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