Purinergic receptor P2Y (P2Y receptor)

Purinergic P2Y receptors are a family of G protein-coupled receptors (GPCRs) that respond to extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose[1][3]. There are at least eight well-characterized subtypes in humans (e.g., P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, P2Y14), each with distinct pharmacology and tissue distribution[2][3][4]. P2Y receptors play key roles in signal transduction, mediating diverse functions such as vasodilation, regulation of blood clotting, vascular growth, immune response, and inflammation[2][3][4][5]. They are widely expressed across tissues and are significant therapeutic targets, with drugs such as clopidogrel and ticagrelor (P2Y12 antagonists) commonly used to prevent thrombosis. P2Y2 agonists (denufosol, diquafosol) are under investigation or approved for diseases like cystic fibrosis and dry eye syndrome[3][6]. Their biological and clinical relevance extends to cardiovascular disease, neurodegeneration, cancer, and inflammatory conditions[2][3][5]. The main therapeutic concern relates to bleeding risk with antiplatelet drugs, and genetic variability affecting drug metabolism can impact clinical outcomes[6][3].

Other names

Purinergic P2Y receptorP2Y receptorP2Y~1~P2Y~2~P2Y~4~P2Y~6~P2Y~11~P2Y~12~P2Y~13~P2Y~14~P2RY (gene family designation)P2RY2Purinergic receptor P2Y, G-protein coupled, [subtype number]

Antagonism/inhibition of P2Y12 to prevent platelet aggregation (thienopyridines) Agonism of P2Y2 to stimulate ion/fluid secretion in epithelia (e.g., dry eye, cystic fibrosis therapies)