Discovery of potent and selective small-molecule PAR-2 agonists

被引：35

作者：

Seitzberg, Jimmi Gerner ^{[1
]}

Knapp, Anne Eeg ^{[1
]}

Lund, Birgitte Winther ^{[1
]}

Bertozzi, Sine Mandrup ^{[1
]}

Currier, Erika A. ^{[2
]}

Ma, Jian-Nong ^{[2
]}

Sherbukhin, Vladimir ^{[1
]}

Burstein, Ethan S. ^{[2
]}

Olsson, Roger ^{[1
]}

机构：

[1] ACADIA Pharmaceut AB, S-20512 Malmo, Sweden

[2] ACADIA Pharmaceut Inc, San Diego, CA 92121 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 18期

关键词：

D O I：

10.1021/jm800754r

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Proteinase activated receptor-2 plays a crucial role in a wide variety of conditions with a strong inflammatory component. We present the discovery and characterization of two structurally different, potent, selective, and metabolically stable small-molecule PAR-2 agonists. These ligands may be useful as pharmacological tools for elucidating the complex physiological role of the PAR-2 receptors as well as for the development of PAR-2 antagonists.

引用

收藏

页码：5490 / 5493

页数：4

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