Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis

…, S Al-Izki, L Clutterbuck, C Posada…

Index: Browne, Lorcan; Lidster, Katie; Al-Izki, Sarah; Clutterbuck, Lisa; Posada, Cristina; Chan, A. W. Edith; Riddall, Dieter; Garthwaite, John; Baker, David; Selwood, David L. Journal of Medicinal Chemistry, 2014 , vol. 57, # 7 p. 2942 - 2952

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Citation Number: 2

Abstract

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 ...