Unità di Medicina 3, Ospedale San Paolo, Dipartimento di Scienze della Salute, Università degli Studi di Milano, Milan, Italy.
Institute of Physiology, Justus-Liebig University Giessen, Giessen, Germany.
J Am Coll Cardiol. 2014 Jun 17;63(23):2503-2509. doi: 10.1016/j.jacc.2014.03.031. Epub 2014 Apr 23.
This review constitutes a critical evaluation of recent publications that have described an additional mode of action of the P2Y12 receptor antagonist ticagrelor. The effect is mediated by inhibition of the adenosine transporter ENT1 (type 1 equilibrative nucleoside transporter), which provides protection for adenosine from intracellular metabolism, thus increasing its concentration and biological activity, particularly at sites of ischemia and tissue injury where it is formed. Understanding the mode of action of ticagrelor is of particular interest given that its clinical profile, both in terms of efficacy and adverse events, differs from that of thienopyridine P2Y12 antagonists.
这篇综述对描述 P2Y12 受体拮抗剂替格瑞洛的另一种作用模式的近期出版物进行了批判性评估。该作用是通过抑制腺苷转运蛋白 ENT1(1 型平衡核苷转运蛋白)介导的,ENT1 可防止腺苷在细胞内代谢,从而增加其浓度和生物活性,特别是在形成部位缺血和组织损伤。鉴于替格瑞洛的临床特征(包括疗效和不良事件)与噻吩吡啶类 P2Y12 拮抗剂不同,因此了解其作用模式尤为重要。