期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 1, 页码 121-124出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.027
关键词
Opioid; kappa Agonist; Active conformation; Conformational analysis
资金
- Shorai Foundation for Science
- Uehara Memorial Foundation
A conformational analysis of kappa opioid receptor agonists, TRK-820 and U-50,488H indicated an active conformation of TRK-820 in which the C-ring was in the boat form with the 14-OH interacting with the amide nitrogen. Based on the obtained active conformation of TRK-820, we designed and synthesized a novel kappa agonist KNT-63 with oxabicyclo[2.2.2]octane skeleton. KNT-63 showed profound antinociceptive effects via the kappa receptor which were as potent as that of TRK-820. (C) 2009 Elsevier Ltd. All rights reserved.
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