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雷诺嗪与晚期心脏钠电流——心绞痛、心律失常及其他疾病的治疗靶点?

Ranolazine and late cardiac sodium current--a therapeutic target for angina, arrhythmia and more?

作者信息

Makielski Jonathan C, Valdivia Carmen R

机构信息

Department of Medicine, Cardiovascular Medicine Section, University of Wisconsin, Madison, WI 53705, USA.

出版信息

Br J Pharmacol. 2006 May;148(1):4-6. doi: 10.1038/sj.bjp.0706713.

DOI:10.1038/sj.bjp.0706713
PMID:16520741
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1617040/
Abstract

Ranolazine is a new antianginal drug approved for clinical use in the United States in January 2006. A study published in this same issue of the British Journal of Pharmacology characterizes ranolazine block of late sodium current caused by the long QT syndrome 3 mutations. This commentary discusses the implications of that study and the background and implications for block of late cardiac sodium current in general.

摘要

雷诺嗪是一种新型抗心绞痛药物,于2006年1月在美国获批用于临床。发表在同一期《英国药理学期刊》上的一项研究描述了雷诺嗪对由长QT综合征3型突变引起的晚钠电流的阻滞作用。本述评讨论了该研究的意义以及心脏晚钠电流阻滞的总体背景和意义。

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Ranolazine and late cardiac sodium current--a therapeutic target for angina, arrhythmia and more?雷诺嗪与晚期心脏钠电流——心绞痛、心律失常及其他疾病的治疗靶点?
Br J Pharmacol. 2006 May;148(1):4-6. doi: 10.1038/sj.bjp.0706713.
2
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本文引用的文献

1
Molecular basis of ranolazine block of LQT-3 mutant sodium channels: evidence for site of action.雷诺嗪对LQT-3突变钠通道的阻滞作用的分子基础:作用位点的证据
Br J Pharmacol. 2006 May;148(1):16-24. doi: 10.1038/sj.bjp.0706709.
2
Cardiac-specific ablation of the Na+-Ca2+ exchanger confers protection against ischemia/reperfusion injury.心脏特异性消融钠钙交换体可提供针对缺血/再灌注损伤的保护作用。
Circ Res. 2005 Oct 28;97(9):916-21. doi: 10.1161/01.RES.0000187456.06162.cb. Epub 2005 Sep 22.
3
Ranolazine CV Therapeutics.雷诺嗪 CV 治疗公司。
Curr Opin Investig Drugs. 2005 Mar;6(3):336-43.
4
Increased late sodium current in myocytes from a canine heart failure model and from failing human heart.来自犬类心力衰竭模型和衰竭人类心脏的心肌细胞中晚期钠电流增加。
J Mol Cell Cardiol. 2005 Mar;38(3):475-83. doi: 10.1016/j.yjmcc.2004.12.012.
5
Electrophysiological effects of ranolazine, a novel antianginal agent with antiarrhythmic properties.雷诺嗪,一种具有抗心律失常特性的新型抗心绞痛药物的电生理效应。
Circulation. 2004 Aug 24;110(8):904-10. doi: 10.1161/01.CIR.0000139333.83620.5D. Epub 2004 Aug 9.
6
Ranolazine: ion-channel-blocking actions and in vivo electrophysiological effects.雷诺嗪:离子通道阻断作用及体内电生理效应。
Br J Pharmacol. 2004 Aug;142(8):1300-8. doi: 10.1038/sj.bjp.0705879. Epub 2004 Jul 26.
7
Antagonism by ranolazine of the pro-arrhythmic effects of increasing late INa in guinea pig ventricular myocytes.雷诺嗪对豚鼠心室肌细胞中晚期钠电流增加所致促心律失常作用的拮抗作用。
J Cardiovasc Pharmacol. 2004 Aug;44(2):192-9. doi: 10.1097/00005344-200408000-00008.
8
Anti-ischemic effects and long-term survival during ranolazine monotherapy in patients with chronic severe angina.雷诺嗪单药治疗慢性重度心绞痛患者的抗缺血作用及长期生存率
J Am Coll Cardiol. 2004 Apr 21;43(8):1375-82. doi: 10.1016/j.jacc.2003.11.045.
9
Antiarrhythmic effects of ranolazine in a guinea pig in vitro model of long-QT syndrome.雷诺嗪对豚鼠长QT综合征体外模型的抗心律失常作用。
J Pharmacol Exp Ther. 2004 Aug;310(2):599-605. doi: 10.1124/jpet.104.066100. Epub 2004 Mar 18.
10
Effects of ranolazine with atenolol, amlodipine, or diltiazem on exercise tolerance and angina frequency in patients with severe chronic angina: a randomized controlled trial.雷诺嗪联合阿替洛尔、氨氯地平或地尔硫䓬对严重慢性心绞痛患者运动耐量和心绞痛发作频率的影响:一项随机对照试验。
JAMA. 2004 Jan 21;291(3):309-16. doi: 10.1001/jama.291.3.309.