Discovery of novel selective Sigma-1 ligands as cognitive enhancers

被引：5

作者：

Valade, Anne ^{[1
]}

Cross, Sophie Binet ^{[2
]}

Brown, Claire ^{[2
]}

Detrait, Eric ^{[1
]}

Ene, Doina ^{[2
]}

Gillard, Michel ^{[1
]}

Guyaux, Michel ^{[1
]}

Lamberty, Yves ^{[1
]}

Maguire, Martin ^{[2
]}

Namdev, Nivedita ^{[2
]}

Provins, Laurent ^{[1
]}

Schwartz, Eric ^{[2
]}

Vermeiren, Celine ^{[1
]}

机构：

[1] UCB NewMed, UCB Pharma, B-1420 Braine Lalleud, Belgium

[2] UCB Res Inc, Cambridge, MA USA

来源：

MEDCHEMCOMM | 2011年 / 2卷 / 07期

关键词：

RECEPTOR-BINDING; PHARMACOLOGY; SA4503;

D O I：

10.1039/c1md00010a

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We disclose the identification and SAR of phenylcyclopropylcarboxamide compounds as novel, selective Sigma-1 ligands presenting excellent drug-like properties, high solubility and metabolic stability. A selected representative, compound 14, demonstrated in vivo very good brain exposure and antiamnesic effect in a mouse model of recognition memory.

引用

页码：655 / 660

页数：6

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