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Synthesis and Optimization of K(v)7 (KCNQ) Potassium Channel Agonists: The Role of Fluorines in Potency and Selectivity

[Image: see text] Based on the potent K(v)7 agonist RL-81, we prepared new lead structures with greatly improved selectivity for K(v)7.2/K(v)7.3 over related potassium channels, i.e., K(v)7.3/K(v)7.5, K(v)7.4, and K(v)7.4/7.5. RL-36 and RL-12 maintain an agonist EC(2x) of ca. 1 μM on K(v)7.2/K(v)7.3...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Liu, Ruiting, Tzounopoulos, Thanos, Wipf, Peter
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6580556/
https://ncbi.nlm.nih.gov/pubmed/31223450
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00097
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