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

页码：697 / 700

页数：4

共 19 条

[1] Selective NMDA NR2B antagonists induce antinociception without motor dysfunction: correlation with restricted localisation of NR2B subunit in dorsal horn [J].