Drug Discovery Opinion

P2X₇ receptors are cation-permeable, ATP-gated ion channels found on cells of immunological origin, including peripheral macrophages and glial cells in the CNS. Studies in P2X₇ receptor knockout mice have suggested a specific role in inflammatory and neuropathic pain states, and there has been considerable interest in developing P2X₇ receptor-selective antagonists for the treatment of inflammatory conditions and pain.

A report in the Oct 22 early edition of PNAS, however, suggests that direct blocking of P2X₇ receptors may not be the best strategy for reducing pain or lessening neuronal degeneration. The report shows that P2X₇ receptors in satellite cells play a crucial role in maintaining proper P2X₃ receptor expression in dorsal root ganglia. Reducing P2X₇ receptor expression using siRNA, or blocking P2X₇ receptor activity by antagonists, was found to cause up-regulation of P2X₃ receptors, leading to increased activity of sensory neurons responding to painful stimuli and evoking abnormal nociceptive behaviours in rats.

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