Discovery of Peripheral κ-Opioid Receptor Agonists as Novel Analgesics

被引：8

作者：

Suzuki, Shinya ^{[1
]}

Sugawara, Yuji ^{[1
]}

Inada, Hideaki ^{[1
]}

Tsuji, Riichiro ^{[1
]}

Inoue, Atsushi ^{[1
]}

Tanimura, Ryuji ^{[1
]}

Shimozono, Rieko ^{[1
]}

Konno, Mitsuhiro ^{[1
]}

Ohyama, Tomofumi ^{[1
]}

Higashi, Eriko ^{[1
]}

Sakai, Chizuka ^{[1
]}

Kawai, Koji ^{[1
]}

机构：

[1] Toray Industries Ltd, Pharmaceut Res Labs, 6-10-1 Tebiro, Kamakura, Kanagawa 2488555, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2017年 / 65卷 / 11期

关键词：

mu-opioid receptor; kappa-opioid receptor; analgesic; TRK-820; 10-ALPHA-HYDROXY; DERIVATIVES; TRK-820;

D O I：

10.1248/cpb.c17-00555

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

kappa-Opioid receptor agonists with high selectivity over the g-opioid receptor and peripheral selectivity are attractive targets in the development of drugs for pain. We have previously attempted to create novel analgesics with peripheral selective kappa-opioid receptor agonist on the basis of TRK-820. In this study, we elucidated the biological properties of 17-hydroxy-cyclopropylmethyl and 10 alpha-hydroxy derivatives. These compounds were found to have better kappa-opioid receptor selectivity and peripheral selectivity than TRK-820.

引用

页码：1085 / 1088

页数：4

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