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ID: ALA1139807

Journal: Bioorg Med Chem Lett

Title: Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.

Authors: Kawai M, Ando K, Matsumoto Y, Sakurada I, Hirota M, Nakamura H, Ohta A, Sudo M, Hattori K, Takashima T, Hizue M, Watanabe S, Fujita I, Mizutani M, Kawamura M.

Abstract: (-)-6-[2-[4-(3-Fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone was identified as an orally active NR2B-subunit selective N-methyl-d-aspartate (NMDA) receptor antagonist. It has very high selectivity for NR2B subunits containing NMDA receptors versus the HERG-channel inhibition (therapeutic index=4200 vs NR2B binding IC(50)). This compound has improved pharmacokinetic properties compared to the prototype CP-101,606.

CiteXplore: 17766106

DOI: 10.1016/j.bmcl.2007.08.014