羟苯氨酮对豚鼠心肌细胞膜Na^+和Ca^(2+)离子通道的影响  

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

作　　者：范礼理[1] 宋珍[1] 王天佑[2] 

机构地区：[1]中国医学科学院,中国协和医科大学药物研究所,北京100050 [2]北京市神经外科研究所,北京100050

出　　处：《药学学报》2004年第6期410-414,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目 ( 3 92 70 778)

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～ 1 0 μmol·L- 1 使电流增加 ,促进钙通道的激活过程 ;2 0与 5 0μmol·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 。Aim To investigate the mechanism of the positive inotropic effect of oxyphenamone. Methods With 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. Results 5-50 μmol·L -1 oxyphenamone 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 -1 oxyphenamone but decreased when the concentration of the drug was elevated to 20-50 μmol·L -1 . Conclusion The 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.

关 键 词：羟苯氨酮 豚鼠 心肌细胞 Na^+离子通道 Ca^2+离子通道 膜片钳 细胞膜 

分 类 号：R972[医药卫生—药品]