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A selective delta opioid receptor antagonist based on a stilbene core
Journal article   Open access   Peer reviewed

A selective delta opioid receptor antagonist based on a stilbene core

Alyssa M Hartung, Hernan A Navarro, David F Wiemer and Jeffrey D Neighbors
Bioorganic & medicinal chemistry letters, Vol.25(23), pp.5532-5535
12/01/2015
DOI: 10.1016/j.bmcl.2015.10.059
PMCID: PMC4645280
PMID: 26525865
url
http://doi.org/10.1016/j.bmcl.2015.10.059View
Open Access

Abstract

[Display omitted] Studies of directed ortho metalation reactions on an aromatic substrate with multiple potential directing groups have identified conditions that favor either of two regioisomers. One of these regioisomers has been converted to an analogue of the stilbene pawhuskin A, and been shown to have high selectivity as an antagonist of the delta opioid receptor. Docking studies have suggested that this compound can adopt a conformation similar to naltrindole, a known delta antagonist.
Pawhuskin Opioid Docking Delta receptor Directed ortho metalation

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