The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function

被引：24

作者：

Jensen, Thomas ^{[1
]}

Elster, Lisbeth ^{[1
]}

Nielsen, Soren Moller ^{[1
]}

Poda, Suresh Babu ^{[1
]}

Loechel, Frosty ^{[1
]}

Volbracht, Christiane ^{[1
]}

Klewe, Ib Vestergaard ^{[1
]}

David, Laurent ^{[1
]}

Watson, Stephen P. ^{[1
]}

机构：

[1] H Lundbeck & Co AS, Neurosci Drug Discovery, DK-2500 Copenhagen, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 22期

关键词：

GPR3; GPR6; GPR12; G protein coupled receptor; Orphan receptor; Inverse agonist; AF64394; ORPHAN RECEPTOR; LIGAND;

D O I：

10.1016/j.bmcl.2014.09.077

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：5195 / 5198

页数：4

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