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Nitazene opioids and the heart: Identification of a cardiac ion channel target for illicit nitazene opioids.
J Mol Cell Cardiol Plus
December 2024
School of Physiology, Pharmacology and Neuroscience, Biomedical Sciences Building, University Walk, Bristol BS8 1TD, UK.
The growing use of nitazene synthetic opioids heralds a new phase of the opioid crisis. However, limited information exists on the toxic effects of these drugs, aside from a propensity for respiratory depression. With restricted research availability of nitazenes, we used machine-learning-based tools to evaluate five nitazene compounds' interaction potential with the hERG potassium channel, a key drug antitarget in the heart.
View Article and Find Full Text PDFCharacterization of novel nitazene recreational drugs: Insights into their risk potential from in vitro µ-opioid receptor assays and in vivo behavioral studies in mice.
Pharmacol Res
December 2024
Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium. Electronic address:
Article Synopsis
- 2-Benzylbenzimidazole derivatives, known as nitazenes, are becoming more prevalent in the recreational drug market, prompting research into their synthesis and effects.
- This study examines 15 different nitazenes, expanding the understanding of their structure-activity relationships and aiding stakeholders like forensic toxicologists and policymakers in managing potential risks.
- Results show that these nitazenes bind strongly to µ-opioid receptors and may have effects similar to or greater than fentanyl, indicating their potential for harm through opioid-like effects observed in mice.
In vitro structure-activity relationships and forensic case series of emerging 2-benzylbenzimidazole 'nitazene' opioids.
Arch Toxicol
September 2024
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 PDFPharmacologic Characterization of Substituted Nitazenes at , , and Opioid Receptors Suggests High Potential for Toxicity.
J Pharmacol Exp Ther
April 2024
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.
View Article and Find Full Text PDF, metabolism and quantification of the novel synthetic opioid N-piperidinyl etonitazene (etonitazepipne).
Clin Chem Lab Med
July 2024
Forensic Toxicology, Institute for Legal Medicine, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Freiburg, Germany.
Objectives: N-piperidinyl etonitazene (etonitazepipne) is a newly synthesized opioid related to the 2-benzylbenzimidazole analog class. Etonitazepipne has been formally notified and placed under intensive monitoring in Europe in January 2022. Nitazenes have high affinity at µ-opioid receptor (MOR).
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