| Literature DB >> 17766106 |
Makoto Kawai1, Kazuo Ando, Yukari Matsumoto, Isao Sakurada, Masako Hirota, Hiroshi Nakamura, Atsuko Ohta, Masaki Sudo, Kazunari Hattori, Tadashi Takashima, Masanori Hizue, Shuzo Watanabe, Isami Fujita, Mayumi Mizutani, Mitsuhiro Kawamura.
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.Entities:
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Year: 2007 PMID： 17766106 DOI： 10.1016/j.bmcl.2007.08.014
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823