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Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands |
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| Authors: | Jason R Healy Padmavani Bezawada Nicholas W Griggs Andrea L Devereaux Rae R Matsumoto John R Traynor Andrew Coop Christopher W Cunningham |
| Institution: | 1. Department of Basic Pharmaceutical Sciences, West Virginia University School of Pharmacy, 2036 Health Sciences North, Morgantown, WV 26506, USA;2. Department of Pharmacology and Experimental Therapeutics, Thomas Jefferson University, 1170 Main Bldg., 132 S. 10th St., Philadelphia, PA 19107, USA;3. Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA;4. Department of Pharmacology, University of Michigan Medical School, 1220A MSRB, Ann Arbor, MI 48109, USA;5. Department of Pharmaceutical Sciences, Concordia University Wisconsin School of Pharmacy, 12800 N. Lake Shore Drive, Mequon, WI 53097, USA;6. Department of Biological and Pharmaceutical Sciences, Touro University California College of Pharmacy, 1310 Club Drive, Vallejo, CA 94592, 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. |
| Keywords: | Mu opioid receptor Delta opioid receptor Analgesic tolerance Oxymorphone Benzylideneoxymorphone |
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