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粉防己碱对心血管电生理特性的影响。

Effects of tetrandrine on cardiovascular electrophysiologic properties.

作者信息

Yao Wei-Xing, Jiang Ming-Xing

机构信息

Department of Pharmacology, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China.

出版信息

Acta Pharmacol Sin. 2002 Dec;23(12):1069-74.

Abstract

Tetrandrine (Tet) is one of the best characterized Ca2+ channel blocker of plant origin. It can affect cardiovascular electrophysiologic properties in following field: inhibit the contractility, +/-dt/dpmax, and automaticity of myocardium, prolong the FRP, and exert concentration-dependent negative inotropic and chronotropic effects without altering cardiac excitability. Tet directly blocks both T-type and L-type calcium current in ventricular cells and vascular smooth muscle cells, but it does not shift the I-V relationship curve of ICa. All its effects would be beneficial in the treatment of angina, arrhythmias, and other cardiovascular disorders. Tet also directly inhibits the activity of BKCa channel in endothelial cell line and also inhibits Ca2+-release-activated channels in vessel endothelial cells, which might significantly contribute to the change of endothelial cell activity.

摘要

粉防己碱(Tet)是植物来源中特征最明确的Ca2+通道阻滞剂之一。它可在以下方面影响心血管电生理特性:抑制心肌收缩力、+/-dt/dpmax和自律性,延长有效不应期(FRP),并产生浓度依赖性负性肌力和变时作用,而不改变心脏兴奋性。粉防己碱直接阻断心室细胞和血管平滑肌细胞中的T型和L型钙电流,但不改变ICa的电流-电压关系曲线。其所有作用对治疗心绞痛、心律失常和其他心血管疾病均有益处。粉防己碱还直接抑制内皮细胞系中BKCa通道的活性,并且抑制血管内皮细胞中Ca2+释放激活通道,这可能显著促成内皮细胞活性的改变。

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