SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as 渭 opioid ligands

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• 作者：Graham Lunn ; Lee R. Roberts ; ^{lee.roberts@pfizer.com} ; Stephane Content ; Douglas J. Critcher ; Sara Douglas ; Ashley E. Fenwick ; David M. Gethin ; Graham Goodwin ; David Greenway ; Sean Greenwood ; Kim Hall ; Martin Thomas ; Stephen Thompson ; David Williams ; Gavin Wood ; Andrew Wylie
• 关键词：渭 Opioid ; Opioid
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March, 2012
• 卷：22
• 期：6
• 页码：2200-2203
• 文件大小：560 K

摘要

3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral 渭 opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting changes to the lead structure which led to compounds having picomolar binding affinity, selective for the 渭 receptor over 未 and 魏 subtypes. Some subtleties of functional activity will also be described.