In Vitro Screening of Opiod Antagonist Effectiveness

Opioid agonists such as fentanyl and its congeners are health risks to members of the U.S. Department of Defense and the general public. Traditionally, opioid overdoses are reversed with an opioid antagonist naloxone Narcan. However, naloxone is reported to be less and less effective at treating overdoses of more potent and new psychoactive substances. One such substance, acrylfentanyl, has been reported to be an irreversible binder of the opioid receptor and thus, Narcan resistant. This study used in vitro methods to test and confirm the nature of ligand receptor interaction by competing the mu-opioid receptor with a co-administration of acrylfentanyl and naloxone. Reversibility of acrylfentanyl was achieved at naloxone concentrations comparable to those of the control compound.