Synthetic opioids have been associated globally with adverse effects in drug users. The nitazene group of drugs is a relatively new addition to the synthetic opioid class emerging in Europe in 2019. Some nitazenes have been shown to be more potent than fentanyl. Overdose clusters in heroin users in Dublin (57 cases) and Cork (20 cases), Ireland, in November and December 2023, respectively, prompted a rapid response from a number of Irish laboratories to identify the substance(s) of concern. Light brown (tan) powders were obtained from cases associated with overdoses, and the results from these analyses by collaboration of four laboratories are reported here. The samples were found to contain N-pyrrolidino protonitazene (protonitazepyne), caffeine, paracetamol, benzoic acid and mannitol.
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In vitro structure-activity relationships and forensic case series of emerging 2-benzylbenzimidazole 'nitazene' opioids.
Arch Toxicol
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Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.
2-Benzylbenzimidazole 'nitazene' opioids are presenting a growing threat to public health. Although various nitazenes were previously studied, systematic comparisons of the effects of different structural modifications to the 2-benzylbenzimidazole core structure on μ-opioid receptor (MOR) activity are limited. Here, we assessed in vitro structure-activity relationships of 9 previously uncharacterized nitazenes alongside known structural analogues.
View Article and Find Full Text PDFIdentification of N-pyrrolidino protonitazene in powders sold as heroin and associated with overdose clusters in Dublin and Cork, Ireland.
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May 2024
Forensic Science Ireland, Dublin, Ireland.
Synthetic opioids have been associated globally with adverse effects in drug users. The nitazene group of drugs is a relatively new addition to the synthetic opioid class emerging in Europe in 2019. Some nitazenes have been shown to be more potent than fentanyl.
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J Pharmacol Exp Ther
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VA Portland Health Care System (L.B.K., A.J.E., K.M.W., T.L.S., S.H.B., S.B., J.L.S., K.A.S., W.E.S., A.J., A.I.A.), Departments of Psychiatry (L.B.K., A.J.E., T.L.S., W.E.S., A.J., A.I.A.), and Behavioral Neuroscience (L.B.K., A.J., A.I.A.), Oregon Health and Science University, Portland, Oregon
The benzimidazole opioids (substituted nitazenes) are highly potent opiod receptor (MOR) agonists with heroin- or fentanyl-like effects. These compounds have caused hospitalizations and fatal overdoses. We characterized the in vitro pharmacology and structure-activity relationships of 19 nitazenes with substitutions at three positions of the benzimidazole core.
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Am J Forensic Med Pathol
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Center for Forensic Science Research and Education at the Fredric Rieders Family Foundation, Willow, Grove, PA.
New generations of novel synthetic opioids (NSOs) have emerged to fill a void in the illicit drug markets left by the decline in popularity of fentanyl analogs subsequent to core-structure scheduling of fentanyl-related substances in the United States and China. These new opioids include members of the 2-benzyl benzimidazole (eg, isotonitazene, metonitazene, N -pyrrolidino etonitazene, protonitazene, etodesnitazene), benzimidazolone (eg, brorphine), and cinnamylpiperazine (eg, AP-238, 2-methyl AP-237) subclasses. Novel synthetic opioids continue to be detected in opioid-related fatal overdoses, demonstrating the harms associated with exposure to these drugs.
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