Browne, L; Lidster, K; Al-Izki, S; Clutterbuck, L; Posada, C; Chan, AE; Riddall, D; ... Selwood, DL; + view all Browne, L; Lidster, K; Al-Izki, S; Clutterbuck, L; Posada, C; Chan, AE; Riddall, D; Garthwaite, J; Baker, D; Selwood, DL; - view fewer (2014) Imidazol-1-ylethylindazole voltage gated sodium (Nav) channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis. J Med Chem , 57 pp. 2942-2952. 10.1021/jm401881q.

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Abstract

A series of imidazol-1-ylethyl)indazole sodium channel ligands were developed and optimized for sodium channel inhibition and in vitro neuroprotective activity. The molecules exhibited displacement of the radiolabelled sodium channel ligand and selectivity for blockade of the inactivated state of cloned neuronal Nav channels. A metabolically stable analogue 6 (CFM6104) was able to protect retinal ganglion cells during optic neuritis in a mouse model of multiple sclerosis.

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