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P2Y12 血小板受体:经皮冠状动脉介入治疗中的重要性。

P2Y12 platelet receptors: importance in percutaneous coronary intervention.

出版信息

Arq Bras Cardiol. 2013 Sep;101(3):277-82. doi: 10.5935/abc.20130162. Epub 2013 Aug 6.

Abstract

Apart from their role in hemostasis and thrombosis, platelets are involved in many other biological processes such as wound healing and angiogenesis. Percutaneous coronary intervention is a highly thrombogenic procedure inducing platelets and monocytes activation through endothelial trauma and contact activation by intravascular devices. Platelet P2Y12 receptor activation by adenosine diphosphate facilitates non-ADP agonist-mediated platelet aggregation, dense granule secretion, procoagulant activity, and the phosphorylation of several intraplatelet proteins, making it an ideal drug target. However, not all compounds that target the P2Y12 receptor have similar efficacy and safety profiles. Despite targeting the same receptor, the unique pharmacologic properties of each of these P2Y12 receptor-directed compounds can lead to very different clinical effects.

摘要

除了在止血和血栓形成中的作用外,血小板还参与许多其他生物学过程,如伤口愈合和血管生成。经皮冠状动脉介入治疗是一种高度血栓形成的过程,通过内皮创伤和血管内装置的接触激活诱导血小板和单核细胞的激活。血小板 P2Y12 受体通过二磷酸腺苷的激活促进非 ADP 激动剂介导的血小板聚集、致密颗粒分泌、促凝活性和几种血小板内蛋白的磷酸化,使其成为理想的药物靶点。然而,并非所有针对 P2Y12 受体的化合物都具有相似的疗效和安全性。尽管针对相同的受体,但这些 P2Y12 受体定向化合物的独特药理学特性可能导致非常不同的临床效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9eb4/4032309/5d44d1147906/abc-101-03-0277-g01.jpg

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