(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.
作者信息
Wu Yong-Jin, Boissard Christopher G, Greco Corinne, Gribkoff Valentin K, Harden David G, He Huan, L'Heureux Alexandre, Kang Shing Hong, Kinney Gene G, Knox Ronald J, Natale Joanne, Newton Amy E, Lehtinen-Oboma Sanna, Sinz Michael W, Sivarao Digavalli V, Starrett John E, Sun Li-Qiang, Tertyshnikova Svetlana, Thompson Mark W, Weaver David, Wong Henry S, Zhang Lei, Dworetzky Steven I
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA.
出版信息
J Med Chem. 2003 Jul 17;46(15):3197-200. doi: 10.1021/jm034073f.
(S)-N-[1-(3-Morpholin-4-ylphenyl)ethyl]-3-phenylacrylamide (2) was synthesized as an orally bioavailable KCNQ2 potassium channel opener. In a rat model of migraine, 2 demonstrated significant oral activity in reducing the total number of cortical spreading depressions induced by potassium chloride.
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