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Published on: September 20, 2016
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands
Jason R Healy1, Padmavani Bezawada2, Nicholas W Griggs3
1Department 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.
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.
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