Design, synthesis, and biological evaluation of C₆-difluoromethylenated epoxymorphinan Mu opioid receptor antagonists

Andrew J. Kassick,Anny Treat,Nestor Tomycz,Michael G. Feasel,Benedict J. Kolber,Saadyah Averick

RSC Medicinal Chemistry（2022）

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摘要

C6-difluoromethylenated epoxymorphinans were found to maintain in vitro potency against fentanyl and displayed effective in vivo blockade of fentanyl-induced anti-nociception in mice relative to the clinical opioid reversal agent naloxone.

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Design, synthesis, and biological evaluation of C6-difluoromethylenated epoxymorphinan Mu opioid receptor antagonists

Design, synthesis, and biological evaluation of C₆-difluoromethylenated epoxymorphinan Mu opioid receptor antagonists