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

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 i...

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Detalles Bibliográficos
Autores principales: Alves, Luiz Anastacio, Bezerra, Rômulo José Soares, Faria, Robson Xavier, Ferreira, Leonardo Gomes Braga, da Silva Frutuoso, Valber
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270334/
https://www.ncbi.nlm.nih.gov/pubmed/24013409
http://dx.doi.org/10.3390/molecules180910953
Descripción
Sumario: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.