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Bioorg Med Chem Lett. 2012 Mar 15;22(6):2200-3. doi: 10.1016/j.bmcl.2012.01.099. Epub 2012 Feb 2.

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

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1
Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK.

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.

PMID:
22357342
DOI:
10.1016/j.bmcl.2012.01.099
[Indexed for MEDLINE]
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