Dipartimento di Scienze della Salute, Università degli Studi di Milano, Unità di Medicina 3, Ospedale San Paolo, Milan, Italy.
J Thromb Haemost. 2015 Jun;13 Suppl 1:S10-6. doi: 10.1111/jth.12952.
The platelet P2Y12 receptor (P2Y12R) for adenosine 5'diphosphate (ADP) plays a central role in platelet function, hemostasis, and thrombosis. Patients with inherited P2Y12R defects display mild-to-moderate bleeding diatheses. Defects of P2Y12R should be suspected when ADP, even at high concentrations (≥ 10 μm), is unable to induce full, irreversible platelet aggregation. P2Y12R also plays a role in inflammation: its role in the pathogenesis of allergic asthma has been well characterized. In addition, inhibition or genetic deficiency of P2Y12R has antitumor effects. Drugs inhibiting P2Y12R are potent antithrombotic drugs. Clopidogrel is the P2Y12R antagonist that is most widely used in the clinical setting. Its most important drawback is its inability to inhibit adequately P2Y12R-dependent platelet function in about one-third of patients. New drugs, such as prasugrel and ticagrelor, which effectively inhibit P2Y12R in the vast majority of patients, have proved to be more efficacious than clopdidogrel in preventing major adverse cardiovascular events.
血小板 P2Y12 受体（P2Y12R）是血小板功能、止血和血栓形成的关键调节因子。患有先天性 P2Y12R 缺陷的患者表现为轻度至中度出血倾向。当 ADP（即使在高浓度下，≥10 μm）无法诱导完全、不可逆的血小板聚集时，应怀疑存在 P2Y12R 缺陷。P2Y12R 在炎症中也发挥作用：其在过敏性哮喘发病机制中的作用已得到充分描述。此外，P2Y12R 的抑制或基因缺失具有抗肿瘤作用。抑制 P2Y12R 的药物是有效的抗血栓形成药物。氯吡格雷是临床应用最广泛的 P2Y12R 拮抗剂。其最重要的缺点是，大约三分之一的患者无法充分抑制 P2Y12R 依赖性血小板功能。新型药物，如普拉格雷和替格瑞洛，可有效地抑制绝大多数患者的 P2Y12R，在预防主要不良心血管事件方面，已被证明比氯吡格雷更有效。
