Recent Patents on Novel P2X7 Receptor Antagonists Potentially Effective for Treatment of Inflammatory Diseases
Affiliation: Gedeon Richter Plc., Laboratory for Molecular Cell Biology, P.O. Box 27, H-1475 Budapest 10, Hungary.
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.
Keywords: Antagonist, inflammation, P2X7 receptor, patent, therapy, P2Z receptor, inflammatory signaling process, neuropathic pain, Neuronal injury, Neuronal degeneration, Diabetic retinopathy, Mood and anxiety disorders
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