Title of article :
(S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo[ and ]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons
Author/Authors :
Yong-Jin Wu، نويسنده , , Christopher G. Boissard، نويسنده , , Jie Chen، نويسنده , , William Fitzpatrick، نويسنده , , Qi Gao، نويسنده , , Valentin K. Gribkoff، نويسنده , , David G. Harden، نويسنده , , Huan He، نويسنده , , Ronald J. Knox، نويسنده , , Joanne Natale، نويسنده , , Rick L. Pieschl، نويسنده , , John E. Starrett Jr.، نويسنده , , Li-Qiang Sun، نويسنده , , Mark Thompson، نويسنده , , David Weaver، نويسنده , , Dedong Wu، نويسنده , , Steven I. Dworetzky، نويسنده ,
Abstract :
(S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-2) was identified as a potent and efficacious KCNQ2 opener. This compound demonstrated significant activity in reducing neuronal hyperexcitability in rat hippocampal slices, and the inhibition mediated by (S)-2 was reversed by the KCNQ blocker linopirdine.
