4-aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists

被引:23
作者
Pinard, E [1 ]
Alanine, A
Bourson, A
Büttelmann, B
Heitz, MP
Mutel, V
Gill, R
Trube, G
Wyler, R
机构
[1] F Hoffmann La Roche Ltd, Div Pharma, Discovery Chem, CH-4070 Basel, Switzerland
[2] F Hoffmann La Roche Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland
关键词
D O I
10.1016/S0960-894X(02)00470-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Screening of the Roche compound library led to the identification of 4-aminoquinoline 4 as structurally novel NR1/2B subtype selective NMDA receptor antagonist. The SAR which was developed in this series resulted in the discovery of highly potent and in vivo active blockers. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2615 / 2619
页数:5
相关论文
共 23 条
[1]  
ALANINE A, 2001, Patent No. 1088818
[2]  
Avdeef A., 1993, APPL THEORY GUIDE PH
[3]   Correlation between 5-HT7 receptor affinity and protection against sound-induced seizures in DBA/2J mice [J].
Bourson, A ;
Kapps, V ;
Zwingelstein, C ;
Rudler, A ;
Boess, FG ;
Sleight, AJ .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1997, 356 (06) :820-826
[4]   Selective NMDA NR2B antagonists induce antinociception without motor dysfunction: correlation with restricted localisation of NR2B subunit in dorsal horn [J].
Boyce, S ;
Wyatt, A ;
Webb, JK ;
O'Donnell, R ;
Mason, G ;
Rigby, M ;
Sirinathsinghji, D ;
Hill, RG ;
Rupniak, NMJ .
NEUROPHARMACOLOGY, 1999, 38 (05) :611-623
[5]   (1S,2S)-1-(4-HYDROXYPHENYL)-2-(4-HYDROXY-4-PHENYLPIPERIDINO)-1-PROPANOL - A POTENT NEW NEUROPROTECTANT WHICH BLOCKS N-METHYL-D-ASPARTATE RESPONSES [J].
CHENARD, BL ;
BORDNER, J ;
BUTLER, TW ;
CHAMBERS, LK ;
COLLINS, MA ;
DECOSTA, DL ;
DUCAT, MF ;
DUMONT, ML ;
FOX, CB ;
MENA, EE ;
MENNITI, FS ;
NIELSEN, J ;
PAGNOZZI, MJ ;
RICHTER, KEG ;
RONAU, RT ;
SHALABY, IA ;
STEMPLE, JZ ;
WHITE, WF .
JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (16) :3138-3145
[6]  
Chenard BL, 1999, CURR PHARM DESIGN, V5, P381
[7]  
FIELD GF, 1985, Patent No. 4560692
[8]  
Fischer G, 1997, J PHARMACOL EXP THER, V283, P1285
[9]  
FISCHER G, 1996, NEUR ANN M WASH DC N
[10]  
Gill R., 1999, CURR OPIN CARDIOVASC, V1, P576