531548-34-2Relevant academic research and scientific papers
Discovery of a series of 2-phenyl- N -(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of Kv7.2 (KCNQ2) channel pharmacology: Identification of (S)-2-phenyl- N -(2-(pyrrolidin-1-yl) phenyl)butanamide (ML252) as a potent, brain penetrant Kv7.2 channel inhibitor
Cheung, Yiu-Yin,Yu, Haibo,Xu, Kaiping,Zou, Beiyan,Wu, Meng,McManus, Owen B.,Li, Min,Lindsley, Craig W.,Hopkins, Corey R.
supporting information; experimental part, p. 6975 - 6979 (2012/09/25)
A potent and selective inhibitor of KCNQ2, (S)-5 (ML252, IC50 = 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, EC50 = 170 nM), suggesting an interaction at a critical site for controlling gating of KCNQ2 channels.
