The P2X₇ receptor as a therapeutic target

Authors: Romagnoli, Romeo; Baraldi, Pier Giovanni; Cruz-Lopez, Olga; Lopez-Cara, Carlota; Preti, Delia; Borea, Pier Andrea; Gessi, Stefania

Source: Expert Opinion on Therapeutic Targets, Volume 12, Number 5, May 2008 , pp. 647-661(15)

Publisher: Informa Healthcare

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Abstract:

Background: The P2X7 receptor is present in a variety of cell types involved in pain, inflammatory processes and neurodegenerative conditions, thus it may be an appealing target for pharmacological intervention. The extensive use of high-throughput screening (HTS) followed by a hit-to-lead (HtL) program, has prompted a number of firms to identify highly selective and metabolically stable small-molecules possessing activity for both the rat and human P2X₇ receptor, which provide a novel therapeutic approach to the treatment of pain as well as neurodegenerative and inflammatory disorders. Objective: To describe the current status of and potential for development of P2X₇ receptor-antagonists. Methods: A literature review. Results/conclusions: We describe the recent discoveries of novel P2X₇ receptor-selective antagonists, along with their biological activity and therapeutic potential.

Keywords: inflammatory process; KN-62; neurodegeneration; neuropathic pain; P2X7 receptor

Document Type: Research article

DOI: http://dx.doi.org/10.1517/14728222.12.5.647

Publication date: 2008-05-01

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