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氯吡格雷和P2Y12受体拮抗剂AR-C69931MX可抑制二磷酸腺苷(ADP)诱导的P-选择素表达及血小板-白细胞结合物形成,而阿司匹林则无此作用。

Inhibition of ADP-induced P-selectin expression and platelet-leukocyte conjugate formation by clopidogrel and the P2Y12 receptor antagonist AR-C69931MX but not aspirin.

作者信息

Storey Robert F, Judge Heather M, Wilcox Robert G, Heptinstall Stan

机构信息

Cardiovascular Medicine, University Hospital, Queen's Medical Centre, Nottingham, UK.

出版信息

Thromb Haemost. 2002 Sep;88(3):488-94.

PMID:12353080
Abstract

Platelet-leukocyte interactions are recognised to have pro-inflammatory effects, which may be important in the pathophysiology of ischaemic heart disease. Clopidogrel and the novel intravenous antithrombotic agent AR-C69931MX act at the level of the platelet P2Y12 receptor, which is known to amplify platelet activation, aggregation and other responses induced by numerous platelet agonists. We studied the effects of clopidogrel and aspirin on ADP-induced platelet-leukocyte conjugate formation and P-selectin expression in healthy volunteers. The effects of clopidogrel and AR-C69931MX administered to patients with ischaemic heart disease were also assessed. AR-C69931MX and aspirin were also studied in vitro. Clopidogrel and AR-C69931MX suppressed ADP-induced platelet aggregation, P-selectin expression and platelet-leukocyte conjugate formation whereas aspirin had no inhibitory effect. These effects of clopidogrel and AR-C69931MX may confer therapeutic benefits in the management of acute coronary syndromes.

摘要

血小板与白细胞的相互作用被认为具有促炎作用,这在缺血性心脏病的病理生理学中可能很重要。氯吡格雷和新型静脉抗血栓药物AR-C69931MX作用于血小板P2Y12受体水平,已知该受体可放大由多种血小板激动剂诱导的血小板活化、聚集及其他反应。我们研究了氯吡格雷和阿司匹林对健康志愿者中ADP诱导的血小板-白细胞结合物形成及P-选择素表达的影响。还评估了氯吡格雷和AR-C69931MX对缺血性心脏病患者的作用。AR-C69931MX和阿司匹林也进行了体外研究。氯吡格雷和AR-C69931MX抑制ADP诱导的血小板聚集、P-选择素表达及血小板-白细胞结合物形成,而阿司匹林无抑制作用。氯吡格雷和AR-C69931MX的这些作用可能在急性冠脉综合征的管理中带来治疗益处。

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