P2X1 purinergic receptor (P2X1)

The P2X1 purinergic receptor is a trimeric, ligand-gated ion channel that is activated by extracellular ATP, mediating rapid influx of cations (primarily calcium and sodium) into target cells. It plays essential roles in smooth muscle contraction, platelet activation, immune cell function, and sperm motility. The receptor is widely expressed in the cardiovascular, urogenital, and immune systems and is being pursued as a therapeutic target for conditions such as thrombosis, inflammation, and male contraception. Drugs have been developed to modulate P2X1 activity, with NF449 as a potent antagonist and α,β-meATP as a selective agonist, although effective clinical translation remains challenging due to issues with target selectivity and rapid receptor desensitization.

Other names

P2X purinoceptor 1P2RX1P2X1 receptorATP-gated ion channel P2X1

Agonists (ATP, α,β-meATP, BzATP): Bind orthosteric sites, open pore, allow cation influx Antagonists (NF449): Block orthosteric site, stabilize closed or inactive conformation, inhibit channel opening