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Activity-based detection and bioanalytical confirmation of a fatal carfentanil intoxication

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Abstract
Carfentaml, one of the most potent opioids known, has recently been reported as a contaminant in street heroin in the United States and Europe, and is associated with an increased number of life-threatening emergency department admissions and deaths. Here, we report on the application of a novel in vitro opioid activity reporter assay and a sensitive bioanalytical assay in the context of a fatal carfentaml intoxication, revealing the highest carfentaml concentrations reported until now. A 21-year-old male was found dead at home with a note stating that he had taken carfentaml with suicidal intentions. A foil bag and plastic bag labeled "C.50" were found at the scene. These bags were similar to a sample obtained by the Belgian Early Warning System on Drugs from a German darknet shop and to those found in the context of a fatality in Norway. Blood, urine and vitreous, obtained during autopsy, were screened with a newly developed in vitro opioid activity reporter assay able to detect compounds based on their mu-opioid receptor activity rather than their chemical structure. All extracts showed strong opioid activity. Results were confirmed by a bioanalytical assay, which revealed extremely high concentrations for carfentaml and norcarfentaml. It should be noted that carfentaml concentrations are typically in pg/mL, but here they were 92 ng/mL in blood, 2.8 ng/mL in urine, and 23 ng/mL in vitreous. The blood and vitreous contained 0.532 and 0.300 ng/mL norcarfentaml, respectively. No norcarfentaml was detected in urine. This is the first report where a novel activity-based opioid screening assay was successfully deployed in a forensic case. Confirmation and quantification using a validated bioanalytical procedure revealed the, to our knowledge, highest carfentaml concentrations reported in humans so far.
Keywords
SYNTHETIC CANNABINOIDS, CASUALTIES, MOSCOW, SERIES, URINE, synthetic opioids, untargeted screening, activity-based, bioassay, carfentanil, LC-MS/MS

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Citation

Please use this url to cite or link to this publication:

Chicago
Cannaert, Annelies, Lars Ambach, Peter Blanckaert, and Christophe Stove. 2018. “Activity-based Detection and Bioanalytical Confirmation of a Fatal Carfentanil Intoxication.” Frontiers in Pharmacology 9.
APA
Cannaert, A., Ambach, L., Blanckaert, P., & Stove, C. (2018). Activity-based detection and bioanalytical confirmation of a fatal carfentanil intoxication. FRONTIERS IN PHARMACOLOGY, 9.
Vancouver
1.
Cannaert A, Ambach L, Blanckaert P, Stove C. Activity-based detection and bioanalytical confirmation of a fatal carfentanil intoxication. FRONTIERS IN PHARMACOLOGY. 2018;9.
MLA
Cannaert, Annelies, Lars Ambach, Peter Blanckaert, et al. “Activity-based Detection and Bioanalytical Confirmation of a Fatal Carfentanil Intoxication.” FRONTIERS IN PHARMACOLOGY 9 (2018): n. pag. Print.
@article{8572587,
  abstract     = {Carfentaml, one of the most potent opioids known, has recently been reported as a contaminant in street heroin in the United States and Europe, and is associated with an increased number of life-threatening emergency department admissions and deaths. Here, we report on the application of a novel in vitro opioid activity reporter assay and a sensitive bioanalytical assay in the context of a fatal carfentaml intoxication, revealing the highest carfentaml concentrations reported until now. A 21-year-old male was found dead at home with a note stating that he had taken carfentaml with suicidal intentions. A foil bag and plastic bag labeled {\textacutedbl}C.50{\textacutedbl} were found at the scene. These bags were similar to a sample obtained by the Belgian Early Warning System on Drugs from a German darknet shop and to those found in the context of a fatality in Norway. Blood, urine and vitreous, obtained during autopsy, were screened with a newly developed in vitro opioid activity reporter assay able to detect compounds based on their mu-opioid receptor activity rather than their chemical structure. All extracts showed strong opioid activity. Results were confirmed by a bioanalytical assay, which revealed extremely high concentrations for carfentaml and norcarfentaml. It should be noted that carfentaml concentrations are typically in pg/mL, but here they were 92 ng/mL in blood, 2.8 ng/mL in urine, and 23 ng/mL in vitreous. The blood and vitreous contained 0.532 and 0.300 ng/mL norcarfentaml, respectively. No norcarfentaml was detected in urine. This is the first report where a novel activity-based opioid screening assay was successfully deployed in a forensic case. Confirmation and quantification using a validated bioanalytical procedure revealed the, to our knowledge, highest carfentaml concentrations reported in humans so far.},
  articleno    = {486},
  author       = {Cannaert, Annelies and Ambach, Lars and Blanckaert, Peter and Stove, Christophe},
  issn         = {1663-9812},
  journal      = {FRONTIERS IN PHARMACOLOGY},
  language     = {eng},
  pages        = {5},
  title        = {Activity-based detection and bioanalytical confirmation of a fatal carfentanil intoxication},
  url          = {http://dx.doi.org/10.3389/fphar.2018.00486},
  volume       = {9},
  year         = {2018},
}

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