Fentanyl is an agonist of the μ-opioid receptor (Ki = 0.39 nM) that less effectively binds the κ-opioid receptor (Ki = 255 nM) and does not act at the δ-opioid receptor.1 It is used for anesthesia and chronic pain management.2,3 Fentanyl, compared to morphine, is both more effective at reducing pain (ED50 values are 0.0061 vs. 0.33 mg/kg, respectively) and more lethal (LD50 values are 62 vs. 470 mg/kg, respectively). 4 Fentanyl is abused recreationally and is regulated as a Schedule II controlled substance in the United States.5
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