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

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• 作者：Jason R. Healy^a ; ^b ; Padmavani Bezawada^c ; Nicholas W. Griggs^d ; Andrea L. Devereaux^e ; Rae R. Matsumoto^a ; ^f ; John R. Traynor^d ; Andrew Coop^c ; Christopher W. Cunningham^e ; ^{chris.cunningham@cuw.edu}
• 关键词：Mu opioid receptor ; Delta opioid receptor ; Analgesic tolerance ; Oxymorphone ; Benzylideneoxymorphone
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：27
• 期：3
• 页码：666-669
• 全文大小：627 K
• 卷排序：27

文摘

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.