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Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis
[Image: see text] 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 inactivat...
| Autores principales: | , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2014
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4010550/ https://www.ncbi.nlm.nih.gov/pubmed/24601592 http://dx.doi.org/10.1021/jm401881q |
| _version_ | 1782479878030884864 |
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| author | Browne, Lorcan Lidster, Katie Al-Izki, Sarah Clutterbuck, Lisa Posada, Cristina Chan, A. W. Edith Riddall, Dieter Garthwaite, John Baker, David Selwood, David L. |
| author_facet | Browne, Lorcan Lidster, Katie Al-Izki, Sarah Clutterbuck, Lisa Posada, Cristina Chan, A. W. Edith Riddall, Dieter Garthwaite, John Baker, David Selwood, David L. |
| author_sort | Browne, Lorcan |
| collection | PubMed |
| description | [Image: see text] 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 Na(v) channels. Metabolically stable analogue 6 was able to protect retinal ganglion cells during optic neuritis in a mouse model of multiple sclerosis. |
| format | Online Article Text |
| id | pubmed-4010550 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-40105502014-05-06 Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis Browne, Lorcan Lidster, Katie Al-Izki, Sarah Clutterbuck, Lisa Posada, Cristina Chan, A. W. Edith Riddall, Dieter Garthwaite, John Baker, David Selwood, David L. J Med Chem [Image: see text] 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 Na(v) channels. Metabolically stable analogue 6 was able to protect retinal ganglion cells during optic neuritis in a mouse model of multiple sclerosis. American Chemical Society 2014-03-06 2014-04-10 /pmc/articles/PMC4010550/ /pubmed/24601592 http://dx.doi.org/10.1021/jm401881q Text en Copyright © 2014 American Chemical Society Terms of Use CC-BY (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) |
| spellingShingle | Browne, Lorcan Lidster, Katie Al-Izki, Sarah Clutterbuck, Lisa Posada, Cristina Chan, A. W. Edith Riddall, Dieter Garthwaite, John Baker, David Selwood, David L. Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis |
| title | Imidazol-1-ylethylindazole
Voltage-Gated Sodium Channel
Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model
of Multiple Sclerosis |
| title_full | Imidazol-1-ylethylindazole
Voltage-Gated Sodium Channel
Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model
of Multiple Sclerosis |
| title_fullStr | Imidazol-1-ylethylindazole
Voltage-Gated Sodium Channel
Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model
of Multiple Sclerosis |
| title_full_unstemmed | Imidazol-1-ylethylindazole
Voltage-Gated Sodium Channel
Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model
of Multiple Sclerosis |
| title_short | Imidazol-1-ylethylindazole
Voltage-Gated Sodium Channel
Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model
of Multiple Sclerosis |
| title_sort | imidazol-1-ylethylindazole
voltage-gated sodium channel
ligands are neuroprotective during optic neuritis in a mouse model
of multiple sclerosis |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4010550/ https://www.ncbi.nlm.nih.gov/pubmed/24601592 http://dx.doi.org/10.1021/jm401881q |
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