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

Lorcan Browne; Katie Lidster; Sarah Al-Izki; Lisa Clutterbuck; Cristina Posada; A. W. Edith Chan; Dieter Riddall; John Garthwaite; David Baker; David L. Selwood

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

机译：咪唑-1-基乙基吲唑电压门控钠通道配体在多发性硬化的小鼠视神经炎过程中具有神经保护作用。

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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.

机译：开发并优化了一系列咪唑-1-基乙基吲唑钠通道配体，以抑制钠通道和体外神经保护活性。该分子表现出放射性标记的钠通道配体的置换和对克隆的神经元Nav通道的失活状态的选择性阻断。代谢稳定的类似物6能够在多发性硬化症小鼠模型中在视神经炎期间保护视网膜神经节细胞。

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《Journal of Medicinal Chemistry》 |2014年第7期|共11页
作者
Lorcan Browne; Katie Lidster; Sarah Al-Izki; Lisa Clutterbuck; Cristina Posada; A. W. Edith Chan; Dieter Riddall; John Garthwaite; David Baker; David L. Selwood;
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正文语种 eng
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关键词
Imidazol-1-ylethylindazole; Voltage-Gated; Sodium Channel Ligands;

机译：咪唑-1-基乙基吲唑;电压门控;钠通道配体;

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1. Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis [J] . Lorcan Browne, Katie Lidster, Sarah Al-Izki, Journal of Medicinal Chemistry . 2014,第7期

机译：咪唑-1-基乙基吲唑电压门控钠通道配体在多发性硬化的小鼠视神经炎过程中具有神经保护作用。
2. Loss of Na+ channel β2 subunits is neuroprotective in a mouse model ofmultiple sclerosis [J] . Heather A. OMalley, Andrew B. Shreiner, Gwo-Hsiao Chen, Molecular and cellular neurosciences . 2009,第2期

机译：Na +通道β2亚基的丧失在多发性硬化症小鼠模型中具有神经保护作用
3. Dynamics of sodium channel Nav1.5 expression in astrocytes in mouse models of multiple sclerosis. [J] . Laura W Pappalardo, Shujun Liu, Joel A Black, Neuroreport . 2014,第15期

机译：多发性硬化小鼠模型中星形胶质细胞钠通道Nav1.5表达的动态。
4. SIMULTANEOUS RECORDING OF VEP AND fMRI TO STUDY OPTIC NEURITIS IN MULTIPLE SCLEROSIS [C] . Muhammad Nabeel Anwar, Laura Bonzano, Davide Rossi-Sebastiano, Biomedical Engineering . 2007

机译：VEP和fMRI同时记录以研究多发性硬化症的视神经炎
5. Neuroprotective Properties of Fingolimod in an Experimental Model of Multiple Sclerosis-Induced Optic Neuritis [D] . Candadai, Amritha Anand. 2020

机译：多发性硬化症诱导视神经炎实验模型中Fingolimod的神经保护性能
6. Imidazol-1-ylethylindazoleVoltage-Gated Sodium ChannelLigands Are Neuroprotective during Optic Neuritis in a Mouse Modelof Multiple Sclerosis [O] . Lorcan Browne, Katie Lidster, Sarah Al-Izki, -1

机译：咪唑-1-基乙基吲唑电压门控钠通道配体在小鼠模型视神经炎期间具有神经保护作用。多发性硬化症
7. Correction to Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis [O] . Lorcan Browne, Katie Lidster, Sarah Al-Izki, 2015

机译：对咪唑-1-萘基唑电压门控钠通道配体的校正是多发性硬化症小鼠模型中的视神经炎期间的神经保护性

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

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