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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Wu, Y.J. et al.

Wu, Boissard, Chen, Fitzpatrick, Gao, Gribkoff, Harden, He, Knox, Natale, Pieschl, Starrett, Sun, Thompson, Weaver, Wu, Dworetzky,

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

(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.[1]

References

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons. Wu, Y.J., Boissard, C.G., Chen, J., Fitzpatrick, W., Gao, Q., Gribkoff, V.K., Harden, D.G., He, H., Knox, R.J., Natale, J., Pieschl, R.L., Starrett, J.E., Sun, L.Q., Thompson, M., Weaver, D., Wu, D., Dworetzky, S.I. Bioorg. Med. Chem. Lett. (2004) [Pubmed]

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