外周κ-阿片受体激动剂作为新型镇痛药的发现。
Discovery of Peripheral κ-Opioid Receptor Agonists as Novel Analgesics.
作者信息
Suzuki Shinya, Sugawara Yuji, Inada Hideaki, Tsuji Riichiro, Inoue Atsushi, Tanimura Ryuji, Shimozono Rieko, Konno Mitsuhiro, Ohyama Tomofumi, Higashi Eriko, Sakai Chizuka, Kawai Koji
机构信息
Pharmaceutical Research Laboratories, Toray Industries, Inc.
出版信息
Chem Pharm Bull (Tokyo). 2017;65(11):1085-1088. doi: 10.1248/cpb.c17-00555.
κ-Opioid receptor agonists with high selectivity over the μ-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 κ-opioid receptor agonist on the basis of TRK-820. In this study, we elucidated the biological properties of 17-hydroxy-cyclopropylmethyl and 10α-hydroxy derivatives. These compounds were found to have better κ-opioid receptor selectivity and peripheral selectivity than TRK-820.
对μ-阿片受体具有高选择性且具有外周选择性的κ-阿片受体激动剂是疼痛药物开发中具有吸引力的靶点。我们之前曾尝试在TRK - 820的基础上创建具有外周选择性κ-阿片受体激动剂的新型镇痛药。在本研究中，我们阐明了17-羟基-环丙基甲基和10α-羟基衍生物的生物学特性。发现这些化合物比TRK - 820具有更好的κ-阿片受体选择性和外周选择性。
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