发现用于逆转神经性疼痛的口服生物可利用的组织蛋白酶S抑制剂。
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
作者信息
Irie Osamu, Kosaka Takatoshi, Ehara Takeru, Yokokawa Fumiaki, Kanazawa Takanori, Hirao Hajime, Iwasaki Astuko, Sakaki Junichi, Teno Naoki, Hitomi Yuko, Iwasaki Genji, Fukaya Hiroaki, Nonomura Kazuhiko, Tanabe Keiko, Koizumi Shinichi, Uchiyama Noriko, Bevan Stuart J, Malcangio Marzia, Gentry Clive, Fox Alyson J, Yaqoob Mohammed, Culshaw Andrew J
机构信息
Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan.
出版信息
J Med Chem. 2008 Sep 25;51(18):5502-5. doi: 10.1021/jm800839j.
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.
组织蛋白酶S抑制剂作为免疫治疗药物是众所周知的有吸引力的靶点。最近，我们的基因表达分析表明，组织蛋白酶S抑制剂对神经性疼痛也可能有效。在此，我们描述了选择性组织蛋白酶S抑制剂在大鼠口服给药后神经性疼痛模型中作为抗痛觉过敏药物的疗效。
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