P2Y1 purinergic receptor (P2Y1)

The P2Y1 purinergic receptor is a member of the purinergic receptor family, classified as a G protein-coupled receptor (GPCR) that is selectively activated by adenosine diphosphate (ADP). It features the canonical seven transmembrane domain structure typical of class A GPCRs. P2Y1 is widely expressed in neuronal, vascular, and gastrointestinal tissues. Functionally, it modulates intracellular calcium release via Gq protein coupling and activates pathways involved in platelet aggregation, neurogenesis, smooth muscle relaxation, and neuroinflammatory responses. The receptor represents an important therapeutic target for a broad array of conditions including cardiovascular disease (e.g., as an antithrombotic), neurodegenerative diseases, cancer, and diabetes. Both agonists and antagonists to P2Y1 are being developed as potential drugs, but therapy must be carefully monitored due to its broad tissue distribution and essential physiological functions.

Other names

P2Y1 receptorPurinergic receptor P2Y1P2RY1

Agonists (e.g., ADP, MRS2365, 2-MeSADP) activate P2Y1, leading to increased intracellular Ca²⁺ signaling, platelet activation, apoptosis in cancer cells, and insulin secretion modulation. Antagonists (e.g., MRS2179) block P2Y1 signaling, leading to decreased platelet aggregation (antithrombotic), neuroprotective effects in TBI/stroke, and modulation of insulin secretion.