P2X7 purinoceptor (P2X7 receptor (P2X7R))

The P2X7 purinoceptor (P2X7 receptor, P2X7R) is an ATP-gated, trimeric ligand-gated ion channel belonging to the P2X receptor family, characterized by two transmembrane domains, intracellular N- and C- termini, and a large extracellular ATP-binding domain[1][2][3]. It is preferentially permeable to cations, especially calcium and sodium, and activation leads to the opening of a pore that can further dilate to allow passage of large molecules[1][5]. Uniquely among P2X receptors, prolonged activation of P2X7 can result in the formation of a membrane pore large enough to allow the entry of molecules up to 900 Da, resulting in cell death or the release of pro-inflammatory mediators. The P2X7 receptor is highly expressed in immune cells and plays a key role in the regulation of inflammation, cytokine release, and apoptosis. Due to its involvement in various pathological processes, including chronic inflammatory diseases, cancer, and neurodegeneration, it is considered an important therapeutic target[3][6]. Multiple antagonists targeting the P2X7 receptor have been developed and studied as potential treatments for these conditions.

Other names

P2X7 receptorP2RX7P2Z receptorATP-gated P2X7 purinoceptorReceptors, Purinergic P2X7

Antagonism of ATP binding, Inhibition of ion channel function, Blockade of large pore formation (by allosteric or orthosteric antagonists)