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Pain; spinal cord injury (SCI)

Purinergic receptor P2X ligand-gated ion channel 4 (P2RX4)

An SAR study identified P2RX4 antagonists that could be useful for treating neuropathic pain and SCI. Genetic inactivation of P2RX4 previously has been shown to reduce inflammatory and neuropathic pain associated with SCI. In a cell culture assay, the lead compound in a series of N-substituted phenoxazines inhibited human P2RX4 with an IC50 value of 0.189 mM and showed 35-fold higher selectively for P2RX4 than for related receptors. Next steps include optimizing potency, selectivity and oral availability of the compounds and evaluating them in mouse models of neuropathic pain.

SciBX 5(44); doi:10.1038/scibx.2012.1167
Published online Nov. 8, 2012

Unpatented; licensing status not applicable

Hernandez-Olmos, V. et al. J. Med. Chem.; published online Oct. 17, 2012;
Contact: Christa E. Müller,
University of Bonn, Bonn, Germany