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Nav1.6 (PN4; SCN8A)

In vitro and mouse studies identified a Nav1.6 inhibitor that could help treat optic neuritis, which is often an initial sign of multiple sclerosis (MS). A series of voltage-dependent sodium channel modulators was designed based on an indazolyloxadiazolyl scaffold. In rat hippocampal slices, the optimal inhibitor targeting Nav1.6 bound the channel with an IC50 value of about 13 mM and produced about 47% neuroprotection at 50 mM under oxygen-glucose deprivation conditions. In a mouse model of MS, the inhibitor prevented loss of retinal nerve cells and decreased optic neuritis symptoms compared with vehicle. Next steps could include testing the inhibitor in additional preclinical models of optic neuritis or MS.

SciBX 7(16); doi:10.1038/scibx.2014.464
Published online April 24, 2014

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Browne, L. et al. J. Med. Chem.; published online March 6, 2014;
Contact: David L. Selwood, University College London, London, U.K.