Abstract
(−)-6-[2-[4-(3-Fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1 H)-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.
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