Recent Patents on Novel P2X7 Receptor Antagonists Potentially Effective for Treatment of Inflammatory Diseases

Involvement of extracellular ATP in inflammatory processes originated in the 1970s when Dahlquist and Diamant reported its histamine releasing action from mast cells. Later a specific ATP receptor was found on these cells, identified as the P2X7 receptor (P2X7R). From these early observations the P2X7R has become increasingly considered as an important regulator of inflammation. Since then, its key role in inflammasome-activated maturation as well as in regulation of the release of several cytokines - including IL-1beta, IL-6, IL-18 and TNF-alpha - has been discovered and widely recognized. Therefore, antagonists of the P2X7 receptor are thought to have therapeutic potential as novel antiinflammatory therapies. The function of the P2X7R in inflammation and its potential role in diseases as well as patent background of its antagonists in the last five years will be reviewed and discussed.