Purinergic P2Y₁₂ receptor (P2Y₁₂ receptor)

The purinergic P2Y₁₂ receptor is a G protein-coupled receptor (GPCR) primarily expressed on platelets and some vascular and immune cells, where it plays a central role in ADP-induced platelet aggregation, hemostasis, and thrombosis[1][5][6]. It is a seven-transmembrane (7TM) domain GPCR activated by nucleotides, especially adenosine diphosphate (ADP). The receptor is the main molecular target of several clinically important antithrombotic drugs (clopidogrel, prasugrel, ticagrelor, and cangrelor), which act by inhibiting ADP-mediated platelet activation and thus reduce thrombotic events such as myocardial infarction and stroke[4][5]. Beyond platelet function, the P2Y₁₂ receptor is implicated in regulation of inflammation and some pathological processes such as asthma and cancer[5]. Genetic variants in P2Y₁₂ can influence drug efficacy and cardiovascular risk, and disruption of its activity may lead to bleeding disorders or altered responses to infection or injury[1][5].

Other names

P2Y12P2Y(12)P2Y₁₂ purinoceptor

Competitive antagonism of ADP binding (inhibits platelet activation/aggregation); Irreversible inhibition (clopidogrel, prasugrel); Reversible inhibition (ticagrelor, cangrelor, AZD1283); Allosteric inhibition/modulation