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

Abstract

The recent widespread abuse of high potency synthetic opioids, such as fentanyl, presents a serious threat to individuals affected by substance use disorder. Synthetic opioids generally exhibit prolonged in vivo...

Are carfentanil and acrylfentanyl naloxone resistant?

“…Two major mechanisms postulating the limitations of standard naloxone antidote dosing, in the event of synthetic opioid poisoning, have been put forward. The renarcotization theory states that the pharmacokinetic mismatch between naloxone and synthetic opioids causes a single naloxone dose to be insufficient at sustained overdose reversal (27)(28)(29)(30)(31)(32)(33). Naloxone resistance is a theorized phenomenon where naloxone has a limited and dulled capacity to reverse synthetic opioid agonist poisoning (22,34).…”