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.
Healy, J. R., Bezawada, P., Griggs, N. W., Devereaux, A. L., Matsumoto, R. R., Traynor, J. R., . . . Cunningham, C. W. (2017). Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands. Bioorganic & Medicinal Chemistry Letters, 27(3), 666-669.
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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