P2X purinoceptor 1 (P2RX1) (P2RX1)

The P2X purinoceptor 1 (P2X1) is a trimeric ligand-gated cation channel that mediates rapid cellular responses to extracellular adenosine triphosphate (ATP) [UniProt: P51575]. It is widely expressed in smooth muscle, platelets, and the central nervous system, where it facilitates the influx of calcium and sodium ions upon activation [PubMed: 10446106]. In the vascular system, P2X1 plays a critical role in platelet activation and thrombus formation, particularly under high-shear stress conditions, positioning it as a target for novel antiplatelet agents [PubMed: 15155816]. Furthermore, P2X1 is essential for the sympathetic contraction of the vas deferens, and its genetic deletion or pharmacological inhibition leads to male infertility, suggesting its potential as a target for non-hormonal male contraception [PubMed: 24302769]. The receptor also contributes to inflammatory responses and bladder function, though its rapid desensitization presents a challenge for therapeutic development [PubMed: 11809864]. Current pharmacological tools include antagonists like NF449 and PPADS, which are primarily used in research to explore the receptor's complex physiology [PubMed: 15606155]. Despite its therapeutic potential, the high degree of homology among P2X subtypes makes achieving selectivity a significant hurdle in drug discovery [PubMed: 11809864].

Other names

P2X1 receptorPurinergic receptor P2X1ATP receptorP2X1

Ligand-gated cation channel that opens upon binding of extracellular ATP, leading to the influx of calcium and sodium ions, resulting in membrane depolarization and intracellular signaling [UniProt: P51575].