title: A potential therapeutic role for P2X7 receptor (P2X7R) antagonists in the treatment of inflammatory diseases.
abstract: BACKGROUND
  The P2X7 receptor (P2X7R) has an important role in inflammation and immunity, but until recently, clinical application has been limited by a lack of specific antagonists. Recent studies using P2X7R knockout mice and specific receptor antagonists have shown that the P2X7R is an important therapeutic target in inflammatory diseases.
  
  
  METHODS
  We have reviewed the current literature on the role of the P2X7R in inflammatory diseases, focusing on potential therapeutic applications of selective P2X7R antagonists as anti-inflammatory agents. Particular emphasis has been placed on the potential role of P2X7R in common inflammatory diseases. The latest developments in Phase I and II clinical trials of P2X7R antagonists are covered.
  
  
  CONCLUSIONS
  Recent studies using gene knockout mice and selective P2X7R antagonists suggest that P2X7R is a viable therapeutic target for inflammatory diseases. However, efficacious P2X7R antagonists for use in clinical studies are still at an early stage of development. Future challenges include: identifying potential toxicity and side effects of treatment, timing of treatment initiation and its duration in chronic inflammatory conditions, optimum dosage and development of a functional assay for P2X7R that would help to guide treatment.
authors.affiliation: Imperial College London, Hammersmith Hospital, Renal Section, Department of Medicine, London, UK.
authors.forename: Nishkantha
authors.initials: N
authors.lastname: Arulkumaran
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Unwin
authors.forename: Frederick Wk
authors.initials: FW
authors.lastname: Tam
mesh_terms: D000818:Animals; D002986:Clinical Trials as Topic / Q000379:methods; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D018836:Inflammation Mediators / Q000378:metabolism / Q000502:physiology / Q000627:therapeutic use*; D058919:Purinergic P2 Receptor Antagonists / Q000378:metabolism / Q000627:therapeutic use*; D058486:Receptors, Purinergic P2X7 / Q000378:metabolism*; D016896:Treatment Outcome
chemical_list: D018836:Inflammation Mediators; D058919:Purinergic P2 Receptor Antagonists; D058486:Receptors, Purinergic P2X7