Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents

被引:108
作者
Burli, Roland W.
Xu, Han
Zou, Xiaoming
Muller, Kristine
Golden, Jennifer
Frohn, Mike
Adlam, Matthew
Plant, Matthew H.
Wong, Min
McElvain, Michele
Regal, Kelly
Viswanadhan, Vellarkad N.
Tagari, Philip
Hungate, Randall
机构
[1] Amgen Inc, Chem Res & Discovery, Thousand Oaks, CA 91320 USA
[2] Amgen Inc, Inflammat, Thousand Oaks, CA 91320 USA
[3] Amgen Inc, Pharmakokinet & Drug Metab, Thousand Oaks, CA 91320 USA
[4] Amgen Inc, Mol Struct, Thousand Oaks, CA 91320 USA
关键词
inflammation; G-protein-coupled receptor; hFPRL1; ALXR; pyrazolones;
D O I
10.1016/j.bmcl.2006.04.068
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 mu M concentration. Recent studies have indicated that agonizing this receptor may promote resolution of inflammation. In an exploratory study, a novel hFPRL1 agonist showed efficacy in a mouse ear inflammation model following oral administration. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3713 / 3718
页数:6
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