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静脉用糖蛋白IIb/IIIa受体阻滞剂的化学结构与作用机制:综述

Chemical structures and mode of action of intravenous glycoprotein IIb/IIIa receptor blockers: A review.

作者信息

Hashemzadeh Mehrnoosh, Furukawa Matthew, Goldsberry Sarah, Movahed Mohammad Reza

机构信息

University of Arizona Sarver Heart Center, Tuscon, Arizona, USA.

出版信息

Exp Clin Cardiol. 2008 Winter;13(4):192-7.

Abstract

Glycoprotein (GP) IIb/IIIa receptor antagonists compose a subcategory of antiplatelet medications that reduce thrombus formation through the blockade of key binding sites needed to stabilize the forming platelet aggregate. The GP IIb/IIIa receptors have been identified as a therapeutic target in reducing the occurrence of platelet-dependent thrombus formation. One advantage of GP IIb/IIIa receptor antagonists is that because GP IIb/IIIa is platelet-specific, inhibition of this receptor does not affect platelet adhesion. This may contribute to hemostasis without leading to ischemic damage. The platelet-specific pharmacological activity of GP IIb/IIIa receptor antagonists has allowed for its broad use in clinical settings. Based on clinical trials, GP IIb/IIIa receptor antagonists have been extensively studied and used in patients with acute coronary syndrome or during percutaneous coronary interventions. The goal of the present article is to provide a detailed review of the chemical structures and mode of action of currently used Food and Drug Administration-approved GP IIb/IIIa receptor antagonists in the United States.

摘要

糖蛋白(GP)IIb/IIIa受体拮抗剂是抗血小板药物的一个亚类,通过阻断稳定正在形成的血小板聚集体所需的关键结合位点来减少血栓形成。GP IIb/IIIa受体已被确定为减少血小板依赖性血栓形成发生的治疗靶点。GP IIb/IIIa受体拮抗剂的一个优点是,由于GP IIb/IIIa是血小板特异性的,抑制该受体不会影响血小板黏附。这可能有助于止血而不会导致缺血性损伤。GP IIb/IIIa受体拮抗剂的血小板特异性药理活性使其能够在临床环境中广泛使用。基于临床试验,GP IIb/IIIa受体拮抗剂已在美国对急性冠状动脉综合征患者或经皮冠状动脉介入治疗期间进行了广泛研究和应用。本文的目的是详细综述美国食品药品监督管理局批准的目前使用的GP IIb/IIIa受体拮抗剂的化学结构和作用方式。

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