Document Type

Article

Publication Date

2017

Publication Title

Bioorganic & Medicinal Chemistry Letters

DOI

10.1016/j.bmcl.2016.11.057

Abstract

Opioid analgesic tolerance remains a considerable drawback to chronic pain management. The finding that concomitant administration of delta opioid receptor (DOR) antagonists attenuates the development of tolerance to mu opioid receptor (MOR) agonists has led to interest in producing bifunctional MOR agonist/DOR antagonist ligands. Herein, we present 7-benzylideneoxymorphone (6, UMB 246) displaying MOR partial agonist/DOR antagonist activity, representing a new lead for designing bifunctional MOR/DOR ligands.

Comments

Please see the work itself for the complete list of authors.

Publisher's Statement

Originally published in Bioorganic & Medicinal Chemistry Letters, 27(3), 666-669. This is an accepted manuscript version of this article. https://doi.org/10.1016/j.bmcl.2016.11.057

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