title: Physiological roles and potential therapeutic applications of the P2X7 receptor in inflammation and pain.
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.
authors.affiliation: Laboratory of Cellular Communication, Oswaldo Cruz Foundation, AV. Brazil 4365, Rio de Janeiro, Brazil. alveslaa@gmail.com
authors.forename: Luiz Anastacio
authors.initials: LA
authors.lastname: Alves
authors.forename: Rômulo José Soares
authors.initials: RJ
authors.lastname: Bezerra
authors.forename: Robson Xavier
authors.initials: RX
authors.lastname: Faria
authors.forename: Leonardo Gomes Braga
authors.initials: LG
authors.lastname: Ferreira
authors.forename: Valber
authors.initials: V
authors.lastname: da Silva Frutuoso
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007249:Inflammation / Q000378:metabolism; D018836:Inflammation Mediators / Q000378:metabolism; D009437:Neuralgia / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism; D059225:Nociception / Q000502:physiology*; D059226:Nociceptive Pain / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism; D058920:Purinergic P2X Receptor Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D058486:Receptors, Purinergic P2X7 / Q000502:physiology*
chemical_list: D000893:Anti-Inflammatory Agents; D018836:Inflammation Mediators; D058920:Purinergic P2X Receptor Antagonists; D058486:Receptors, Purinergic P2X7