Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
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DOI：
10.1021/jm401881q
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发表时间：
2014-04-10
影响因子：
7.3
通讯作者：
Selwood DL
中科院分区：
文献类型：
--
作者：
Browne L;Lidster K;Al-Izki S;Clutterbuck L;Posada C;Chan AW;Riddall D;Garthwaite J;Baker D;Selwood DL
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.
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