Discovery of a Series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as Novel Molecular Switches that Modulate Modes of K(v)7.2 (KCNQ2) Channel Pharmacology: Identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a Potent, Brain Penetrant K(v)7.2 Channel Inhibitor

A potent and selective inhibitor of KCNQ2, (S)-5 (ML252, IC(50) = 69 nM), was discovered after a high-throughput screen of the MLPCN library was performed. SAR studies revealed a small structural change (ethyl group to hydrogen) caused a functional shift from antagonist to agonist activity (37, EC(5...

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Main Authors: Cheung, Yiu-Yin, Yu, Haibo, Xu, Kaiping, Zou, Beiyan, Wu, Meng, McManus, Owen B., Li, Min, Lindsley, Craig W., Hopkins, Corey R.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3530927/
https://ncbi.nlm.nih.gov/pubmed/22793372
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300700v
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