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REGULATION OF PLATELET FUNCTIONS BY P2 RECEPTORS

2006/02/01 by Christian Gachet

paper · doi:10.1146/annurev.pharmtox.46.120604.141207

Abstract

▪ Abstract The main role of blood platelets is to ensure primary hemostasis, which is the maintenance of vessel integrity and cessation of bleeding upon injury. While playing a major part in acute arterial thrombosis, platelets are also involved in inflammation, atherosclerosis, and angiogenesis. ADP and ATP play a crucial role in platelet activation, and their receptors are potential targets for antithrombotic drugs. The ATP-gated cation channel P2X 1 and the two G protein–coupled ADP receptors, P2Y 1 and P2Y 12 , selectively contribute to platelet aggregation and formation of a thrombus. Owing to its central role in the growth and stabilization of a thrombus, the P2Y 12 receptor is an established target of antithrombotic drugs such as clopidogrel. Studies in P2Y 1 and P2X 1 knockout mice and selective P2Y 1 and P2X 1 antagonists have shown that these receptors are also attractive targets for new antithrombotic compounds. The potential role of platelet P 2 receptors in the involvement of platelets in inflammatory processes is also discussed.

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