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Imidazol-1-ylethylindazole voltage gated sodium (Nav) channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.

Browne, L; Lidster, K; Al-Izki, S; Clutterbuck, L; Posada, C; Chan, AE; Riddall, D; ... Selwood, DL; + view all (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. Green open access

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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.

Type: Article
Title: Imidazol-1-ylethylindazole voltage gated sodium (Nav) channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
Open access status: An open access version is available from UCL Discovery
DOI: 10.1021/jm401881q
Publisher version: http://dx.doi.org/10.1021/jm401881q
Language: English
Additional information: Copyright © 2014 American Chemical Society ACS AuthorChoice - Terms of Use CC-BY PMCID: PMC4010550
UCL classification: UCL
UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Department of Education
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Wolfson Inst for Biomedical Research
URI: https://discovery.ucl.ac.uk/id/eprint/1423606
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