Molecules 2013, 18(9), 10953-10972; doi:10.3390/molecules180910953
Review

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

1,* email, 1email, 1email, 1email and 2email
Received: 17 June 2013; in revised form: 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)
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Abstract: 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.
Keywords: P2X7R; inflammatory response; antagonists and pharmacological target
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

Alves LA, Bezerra RJS, Faria RX, Ferreira LGB, da Silva Frutuoso V. Physiological Roles and Potential Therapeutic Applications of the P2X7 Receptor in Inflammation and Pain. Molecules. 2013; 18(9):10953-10972.

Chicago/Turabian Style

Alves, Luiz A.; Bezerra, Rômulo J.S.; Faria, Robson X.; Ferreira, Leonardo G.B.; da Silva Frutuoso, Valber. 2013. "Physiological Roles and Potential Therapeutic Applications of the P2X7 Receptor in Inflammation and Pain." Molecules 18, no. 9: 10953-10972.


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