Platelet P2Y12 receptor (P2Y12)

The platelet P2Y12 receptor is a GPCR located on the surface of platelets, critically involved in amplifying and sustaining ADP-induced platelet activation, aggregation, shape change, and degranulation in the hemostatic process. Its activation by ADP leads to G_i protein-mediated inhibition of adenylyl cyclase, decreasing intracellular cAMP and activating downstream pathways including phosphoinositide 3-kinase and potassium channels. Therapies targeting the P2Y12 receptor (notably clopidogrel, prasugrel, and ticagrelor) prevent arterial thrombosis and are central to acute coronary syndrome management. The receptor also plays roles in pathological conditions including bleeding disorders (when defective), inflammation, some cancers, and allergic asthma. Safety concerns primarily relate to increased bleeding risk and variable response to clopidogrel.

Other names

P2Y12 purinoceptorP2Y12R

Antagonists inhibit ADP binding, preventing G_i protein signaling, leading to reduced platelet aggregation, degranulation, and thrombus formation