| Literature DB >> 22357342 |
Graham Lunn1, Lee R Roberts, 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.
Abstract
3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral μ 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 μ receptor over δ and κ subtypes. Some subtleties of functional activity will also be described. Copyright ÂEntities:
Mesh：
Substances：
Year: 2012 PMID： 22357342 DOI： 10.1016/j.bmcl.2012.01.099
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823