Gachet C
INSERM U311, Etablissement Français du Sang-Alsace, Strasbourg, France.
Thromb Haemost. 2001 Jul;86(1):222-32.
ADP plays a crucial role in haemostasis and thrombosis and its receptors are potential targets for antithrombotic drugs. Two G-protein coupled P2 receptors contribute to platelet aggregation: the P2Y1 receptor initiates aggregation through mobilisation of calcium stores, while the more recently identified P2Y12 receptor coupled to adenylyl cyclase inhibition is essential for a full aggregation response to ADP and the stabilisation of aggregates. The latter is defective in certain patients with a selective congenital deficiency of aggregation to ADP. It is also the target of the antithrombotic drug clopidogrel and of ATP analogues and other compounds currently under evaluation. In addition, the P2X1 ionotropic receptor is present in platelets but its role is not yet completely known. Studies in P2Y1 knock-out mice and experimental thrombosis models using selective P2Y1 antagonists have shown that the P2Y1 receptor, like the P2Y12 receptor, is a potential target for new antithrombotic drugs.
二磷酸腺苷（ADP）在止血和血栓形成过程中发挥着关键作用，其受体是抗血栓药物的潜在靶点。两种G蛋白偶联P2受体参与血小板聚集：P2Y1受体通过动员钙库启动聚集，而最近发现的与腺苷酸环化酶抑制偶联的P2Y12受体对于ADP的完全聚集反应和聚集体的稳定至关重要。在某些先天性选择性ADP聚集缺陷患者中，后者存在缺陷。它也是抗血栓药物氯吡格雷以及目前正在评估的ATP类似物和其他化合物的作用靶点。此外，P2X1离子型受体存在于血小板中，但其作用尚未完全明确。对P2Y1基因敲除小鼠的研究以及使用选择性P2Y1拮抗剂的实验性血栓形成模型表明，与P2Y12受体一样，P2Y1受体也是新型抗血栓药物的潜在靶点。
