Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain

被引：33

作者：

Irie, Osamu ^{[1
]}

Kosaka, Takatoshi ^{[1
]}

Ehara, Takeru ^{[1
]}

Yokokawa, Fumiaki ^{[1
]}

Kanazawa, Takanori ^{[1
]}

Hirao, Hajime ^{[1
]}

Iwasaki, Astuko ^{[1
]}

Sakaki, Junichi ^{[1
]}

Teno, Naoki ^{[1
]}

Hitomi, Yuko ^{[1
]}

Iwasaki, Genji ^{[1
]}

Fukaya, Hiroaki ^{[1
]}

Nonomura, Kazuhiko ^{[1
]}

Tanabe, Keiko ^{[1
]}

Koizumi, Shinichi ^{[1
]}

Uchiyama, Noriko ^{[1
]}

Bevan, Stuart J. ^{[1
]}

Malcangio, Marzia ^{[2
]}

Gentry, Clive ^{[2
]}

Fox, Alyson J. ^{[2
]}

Yaqoob, Mohammed ^{[2
]}

Culshaw, Andrew J. ^{[2
]}

Hallett, Allan ^{[2
]}

机构：

[1] Novartis Inst BioMed Res, Tsukuba, Ibaraki 3002611, Japan

[2] Novartis Inst BioMed Res, London WC1E 6BS, England

来源：

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

关键词：

D O I：

10.1021/jm800839j

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cathepsin S inhibitors are well-known to be an attractive target as immunological therapeutic agents. Recently, Our gene expression analysis identified that cathepsin S inhibitors could also be effective for neuropathic pain. Herein, we describe the efficacy of selective cathepsin S inhibitors as antihyperalgesics in a model of neuropathic pain in rats after oral administration.

引用

页码：5502 / 5505

页数：4

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