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Molecules 2013, 18(9), 10953-10972;

Physiological Roles and Potential Therapeutic Applications of the P2X7 Receptor in Inflammation and Pain

Laboratory of Cellular Communication, Oswaldo Cruz Foundation, AV. Brazil, 4365, Rio de Janeiro, Brazil
Laboratory of Immnopharmacology, Oswaldo Cruz Foundation, AV. Brazil 4365, Rio de Janeiro, Brazil
Author to whom correspondence should be addressed.
Received: 17 June 2013 / Revised: 26 August 2013 / Accepted: 27 August 2013 / Published: 5 September 2013
(This article belongs to the Special Issue Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry)
Full-Text   |   PDF [218 KB, uploaded 18 June 2014]


The P2X7 receptor (P2X7R) is a nonselective cation channel that is activated by extracellular ATP and triggers the secretion of several proinflammatory substances, such as IL-1β, IL-18, TNF-α, and nitric oxide. Recently, several preclinical studies have demonstrated that this receptor participates in inflammation and pain mechanisms. Taken together, these results indicate that P2X7R is a promising pharmacological target, and compounds that modulate the function of this receptor show potential as new anti-inflammatory medicines. In this review, we discuss aspects of P2X7R pharmacology and the participation of this protein in inflammation and pain and provide an overview of some promising compounds that have been tested as antagonists of P2X7R, with clinical applicability. View Full-Text
Keywords: P2X7R; inflammatory response; antagonists and pharmacological target P2X7R; inflammatory response; antagonists and pharmacological target
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Alves, L.A.; Bezerra, R.J.S.; Faria, R.X.; Ferreira, L.G.B.; Da Silva Frutuoso, V. Physiological Roles and Potential Therapeutic Applications of the P2X7 Receptor in Inflammation and Pain. Molecules 2013, 18, 10953-10972.

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