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.

Kawai, Makoto; Ando, Kazuo; Matsumoto, Yukari; Sakurada, Isao; Hirota, Masako; Nakamura, Hiroshi; Ohta, Atsuko; Sudo, Masaki; Hattori, Kazunari; Takashima, Tadashi; Hizue, Masanori; Watanabe, Shuzo; Fujita, Isami; Mizutani, Mayumi; Kawamura, Mitsuhiro

Kawai, Makoto; Ando, Kazuo; Matsumoto, Yukari; Sakurada, Isao; Hirota, Masako; Nakamura, Hiroshi; Ohta, Atsuko; Sudo, Masaki; Hattori, Kazunari; Takashima, Tadashi; Hizue, Masanori; Watanabe, Shuzo; Fujita, Isami; Mizutani, Mayumi; Kawamura, Mitsuhiro.

Affiliation

Kawai M; Discovery Chemistry, Pfizer Global Research & Development, Nagoya laboratories, 5-2 Taketoyo, Aichi 470-2393, Japan.

Bioorg Med Chem Lett ; 17(20): 5558-62, 2007 Oct 15.

Article in En | MEDLINE | ID: mdl-17766106

Subject(s)

N-Methylaspartate/antagonists & inhibitors; N-Methylaspartate/metabolism; Pain; Piperidines/chemistry; Quinolones/chemistry; Receptors, N-Methyl-D-Aspartate/metabolism; Animals; Cytochrome P-450 CYP2D6/metabolism; Cytochrome P-450 CYP2D6 Inhibitors; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Ether-A-Go-Go Potassium Channels/metabolism; Inhibitory Concentration 50; Molecular Structure; Pain/drug therapy; Piperidines/pharmacology; Quinolones/pharmacology; Rats; Structure-Activity Relationship

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Collection: 01-internacional Database: MEDLINE Main subject: Pain / Piperidines / N-Methylaspartate / Receptors, N-Methyl-D-Aspartate / Quinolones Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2007 Document type: Article Affiliation country: Japan Country of publication: United kingdom

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