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Bioorg Med Chem Lett
; 21(15): 4608-11, 2011 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-21737265
ABSTRACT
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-fold improvement in binding. An early example from the series had excellent µ opioid receptor antagonist antagonist activity and was very effective in an in vivo pruritus study.