Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
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ABSTRACT:
SUBMITTER: Browne L
PROVIDER: S-EPMC4010550 | biostudies-literature | 2014 Apr
REPOSITORIES: biostudies-literature
Publications
Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
Browne Lorcan L Lidster Katie K Al-Izki Sarah S Clutterbuck Lisa L Posada Cristina C Chan A W Edith AW Riddall Dieter D Garthwaite John J Baker David D Selwood David L DL
Journal of medicinal chemistry 20140321 7
A series of imidazol-1-ylethylindazole sodium channel ligands were developed and optimized for sodium channel inhibition and in vitro neuroprotective activity. The molecules exhibited displacement of a radiolabeled sodium channel ligand and selectivity for blockade of the inactivated state of cloned neuronal Nav channels. Metabolically stable analogue 6 was able to protect retinal ganglion cells during optic neuritis in a mouse model of multiple sclerosis. ...[more]
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