Orally efficacious NR2B-selective NMDA receptor antagonists

被引：51
|
作者：
Claiborne, CF
McCauley, JA [1 ]
Libby, BE
Curtis, NR
Diggle, HJ
Kulagowski, JJ
Michelson, SR
Anderson, KD
Claremon, DA
Freidinger, RM
Bednar, RA
Mosser, SD
Gaul, SL
Connolly, TM
Condra, CL
Bednar, B
Stump, GL
Lynch, JJ
Macaulay, A
Wafford, KA
Koblan, KS
Liverton, NJ
机构：
[1] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA
[2] Merck Sharp & Dohme Res Labs, Dept Med Chem, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England
[3] Merck Res Labs, Dept Mol Pharmacol, W Point, PA 19486 USA
[4] Merck Sharp & Dohme Res Labs, Dept Pharmacol, W Point, PA 19486 USA
[5] Merck Sharp & Dohme Res Labs, Dept Pharmacol, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 04期
关键词：
D O I：
10.1016/S0960-894X(02)01061-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of benzamidines as synthesized and shogun to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：697 / 700
页数：4
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