280760-64-7Relevant academic research and scientific papers
SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as μ opioid ligands
Lunn, Graham,Roberts, Lee R.,Content, Stephane,Critcher, Douglas J.,Douglas, Sara,Fenwick, Ashley E.,Gethin, David M.,Goodwin, Graham,Greenway, David,Greenwood, Sean,Hall, Kim,Thomas, Martin,Thompson, Stephen,Williams, David,Wood, Gavin,Wylie, Andrew
scheme or table, p. 2200 - 2203 (2012/05/04)
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
Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a 'magic methyl' giving a 35-fold improvement in binding
Lunn, Graham,Banks, Bernard J.,Crook, Robert,Feeder, Neil,Pettman, Alan,Sabnis, Yogesh
, p. 4608 - 4611 (2011/09/15)
In looking for a novel achiral μ opioid receptor antagonist for the treatment of pruritus, we designed and synthesised azabicyclo[3.1.0]hexane compounds as a new class of opioid ligand. During optimisation, an addition of a single methyl resulted in a 35-
