( 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
Journal of Medicinal Chemistry2003Vol. 46(15), pp. 3197–3200
Citations Over TimeTop 23% of 2003 papers
Yong‐Jin Wu, Christopher G. Boissard, Corinne Greco, Valentin K. Gribkoff, David Harden, Huan He, Alexandre L’Heureux, Shing Hong Kang, Gene G. Kinney, Ronald J. Knox, Joanne Natale, Amy Newton, Sanna Lehtinen-Oboma, Michael Sinz, Digavalli V. Sivarao, John E. Starrett, Li‐Qiang Sun, Svetlana Tertyshnikova, Mark Thompson, David T. Weaver, Henry S. Wong, Lei Zhang, Steven I. Dworetzky
Abstract
(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.