The Physiology, Pharmacology and Future of P2X7 as An Analgesic Drug Target: Hype or Promise?

Anindya      Bhattacharya; Robert      A. Neff; Alan      D. Wickenden

Abstract

P2X7 is an ATP-gated non-selective cation channel expressed primarily on cells of hematopoietic origin, such as macrophages and microglia. Since the initial cloning of this channel, enormous progress has been made in the understanding of the physiology, pharmacology and therapeutic utility of P2X7. This article attempts to review the biology of P2X7 with a focus on the complex pharmacology of this channel. Finally, the authors discuss the role of P2X7 as an analgesic drug target and raise some of the challenges and issues that face the P2X7 research community.

Keywords: P2X7, pain, IL-1β, inflammation, purinergic, ATP-gated non-selective cation channel, hematopoietic origin, macrophages, microglia, therapeutic utility of P2X7, Analgesic Drug Target, ATP gated ion channels, nonselective flux, currentvoltage relationship, P2X7 ACTIVATION AND MATURE IL-1 RELEASE