Acrylfentanyl (also known asacryloylfentanyl) is a highly potentopioidanalgesic that is ananalog offentanyl and has been sold online as adesigner drug.[1][2][3][4][5] In animal studies theIC50 (the half maximal inhibitory concentration for acrylfentanyl to displacenaloxone) is 1.4 nM, being slightly more potent than fentanyl itself (1.6 nM) as well as having a longer duration of action.[6][7][8][9]
Side effects offentanyl analogs are similar to those of fentanyl itself, which includeitching,nausea and potentially seriousrespiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.[10]
Asacrylamide derivatives are often used indrug discovery to make covalent inhibitors which will bind irreversibly to its target, acrylfentanyl is claimed to be naloxone resistant.[11] However, acute intoxications with acrylfentanyl on mice[12] treated by naloxone (2 mg/kg) have shown that acrylfentanyl could be displaced from the opioid receptor.
Acrylfentanyl has been linked to 20 deaths in Sweden as well as two deaths in Denmark in summer 2016.[13][14]
^Ujváry I, Jorge R, Christie R, Le Ruez T, Danielsson HV, Kronstrand R, Elliott S, Gallegos A, Sedefov R, Evans-Brown M (July 2017). "Acryloylfentanyl, a recently emerged new psychoactive substance: a comprehensive review".Forensic Toxicology.35 (2):232–243.doi:10.1007/s11419-017-0367-8.S2CID30184205.
^Maryanoff BE, Simon EJ, Gioannini T, Gorissen H (August 1982). "Potential affinity labels for the opiate receptor based on fentanyl and related compounds".Journal of Medicinal Chemistry.25 (8):913–919.doi:10.1021/jm00350a006.PMID6288945.
^Essawi MY (April 1999). "Fentanyl analogues with a modified propanamido group as potential affinity labels: synthesis and in vivo activity".Die Pharmazie.54 (4):307–308.PMID10234745.
^Mounteney J, Giraudon I, Denissov G, Griffiths P (July 2015). "Fentanyls: Are we missing the signs? Highly potent and on the rise in Europe".The International Journal on Drug Policy.26 (7):626–631.doi:10.1016/j.drugpo.2015.04.003.PMID25976511.
^Maryanoff BE, Simon EJ, Gioannini T, Gorissen H (August 1982). "Potential affinity labels for the opiate receptor based on fentanyl and related compounds".Journal of Medicinal Chemistry.25 (8):913–919.doi:10.1021/jm00350a006.PMID6288945.
^"Akrylfentanyl narkotikaklassas" [Acrylfentanyl is classified as a drug].Rättsmedicinalverket [Forensic Medicine Agency] (in Swedish). 9 August 2016.
