In vitro activity-profiling of Cumyl-PEGACLONE variants at the CB1 receptor: fluorination versus isomer exploration.

  title={In vitro activity-profiling of Cumyl-PEGACLONE variants at the CB1 receptor: fluorination versus isomer exploration.},
  author={Liesl K Janssens and Annelies Cannaert and Matthew J. Connolly and Huiling Liu and Christophe P. Stove},
  journal={Drug testing and analysis},
Synthetic cannabinoid receptor agonists (SCRAs) are one of the largest groups of new psychoactive substances (NPS) monitored in Europe. SCRAs are known to typically exert higher cannabinoid activity than THC from cannabis, therefore entailing a greater health risk. Both Cumyl-PEGACLONE and 5F-Cumyl-PEGACLONE were not controlled by the national legislation upon their first detection in Germany in 2016 and 2017, respectively, and have been linked to several fatalities. In this study, the CB1… 
8 Citations
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A new G-protein coupled receptor (GPCR) activation assay based on NanoLuc binary technology is developed and applied, and it is demonstrated that several major metabolites of these SCs retain their activity at cannabinoid receptors.
Structural characterization and pharmacological evaluation of the new synthetic cannabinoid CUMYL-PEGACLONE.
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Human phase I metabolism of the novel synthetic cannabinoid 5F-CUMYL-PEGACLONE
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Hypothermia was reversed by pretreatment with a CB1, but not CB2, antagonist, confirming that cumyl-derived SCs are cannabimimetic in vivo.