Purinergic receptor P2X(7): A novel target for anti-inflammatory therapy

Purinergic receptors, also known as purinoceptors, are ligand gated membrane ion channels involved in many cellular functions. Among all identified purinergic receptors, P2X(7) subform is unique since it induces the caspase activity, cytokine secretion, and apoptosis. The distribution of P2X(7) receptors, and the need of high concentration of ATP required to activate this receptor exhibited its ability to function as 'danger' sensor associated with tissue inflammation and damage. Further, the modulation of other signalling pathways associated with P2X(7) has also been proposed to play an important role in the control of macrophage functions and inflammatory responses, especially towards lipopolysaccharides. Experimentally, researchers have also observed the decreased severity of inflammatory responses in P2X(7) receptor expressing gene (P2RX7) knockout (KO) phenotypes. Therefore, newly developed potent antagonists of P2X(7) receptor would serve as novel therapeutic agents to combat various inflammatory conditions. In this review article, we tried to explore various aspects of P2X(7) receptors including therapeutic potential, and recent discoveries and developments of P2X(7) receptor antagonists. (C) 2013 Elsevier Ltd. All rights reserved.