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Bioorg Med Chem Lett. 2017 Feb 1;27(3):666-669. doi: 10.1016/j.bmcl.2016.11.057. Epub 2016 Nov 22.

Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.

Author information

1
Department of Basic Pharmaceutical Sciences, West Virginia University School of Pharmacy, 2036 Health Sciences North, Morgantown, WV 26506, USA; Department of Pharmacology and Experimental Therapeutics, Thomas Jefferson University, 1170 Main Bldg., 132 S. 10th St., Philadelphia, PA 19107, USA.
2
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA.
3
Department of Pharmacology, University of Michigan Medical School, 1220A MSRB, Ann Arbor, MI 48109, USA.
4
Department of Pharmaceutical Sciences, Concordia University Wisconsin School of Pharmacy, 12800 N. Lake Shore Drive, Mequon, WI 53097, USA.
5
Department of Basic Pharmaceutical Sciences, West Virginia University School of Pharmacy, 2036 Health Sciences North, Morgantown, WV 26506, USA; Department of Biological and Pharmaceutical Sciences, Touro University California College of Pharmacy, 1310 Club Drive, Vallejo, CA 94592, USA.
6
Department of Pharmaceutical Sciences, Concordia University Wisconsin School of Pharmacy, 12800 N. Lake Shore Drive, Mequon, WI 53097, USA. Electronic address: chris.cunningham@cuw.edu.

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.

KEYWORDS:

Analgesic tolerance; Benzylideneoxymorphone; Delta opioid receptor; Mu opioid receptor; Oxymorphone

PMID:
28011222
PMCID:
PMC5404377
DOI:
10.1016/j.bmcl.2016.11.057
[Indexed for MEDLINE]
Free PMC Article

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