In-depth comparison of the metabolic and pharmacokinetic behaviour of the structurally related synthetic cannabinoids AMB-FUBINACA and AMB-CHMICA in rats
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Synthetic cannabinoids receptor agonists (SCRAs) are often almost completely metabolised, and hence their pharmacokinetics should be carefully evaluated for determining the most adequate biomarker in toxicological analysis. Two structurally related SCRAs, AMB-FUBINACA and AMB-CHMICA, were selected to evaluate their in vivo metabolism and pharmacokinetics using male Sprague-Dawley rats. Brain, liver, kidney, blood (serum) and urine samples were collected at different times to assess the differences in metabolism, metabolic reactions, tissue distribution and excretion. Both compounds experimented O-demethyl reaction, which occurred more rapidly for AMB-FUBINACA. The parent compounds and O-demethyl metabolites were highly bioaccumulated in liver, and were still detected in this tissue 48 h after injection. The different indazole/indole N-functionalisation produced diverse metabolic reactions in this moiety and thus, different urinary metabolites were formed. Out of the two compounds, AMB-FUBINACA seemed to easily cross the blood-brain barrier, presenting higher brain/serum concentrations ratio than AMB-CHMICA.
| Original language | English |
|---|---|
| Article number | 161 |
| Journal | Communications Biology |
| Volume | 5 |
| Issue number | 1 |
| Number of pages | 13 |
| ISSN | 2399-3642 |
| DOIs | |
| Publication status | Published - 2022 |
Bibliographical note
Funding Information:
D. Fabregat-Safont, J.V. Sancho, F. Hern?ndez and M. Ib??ez acknowledge financial support from the Generalitat Valenciana (PROMETEO/2019/040) and the University Jaume I (UJI-B2018-19). D. Fabregat-Safont acknowledges Ministerio de Educaci?n, Cultura y Deporte in Spain for his predoctoral grant (FPU15/02033). M. Mata-Pesquera acknowledges Ministerio de Educaci?n y Formaci?n Profesional in Spain for her undergraduate research grant (998142). F. Martinez-Garcia and M. Barneo-Mu?oz acknowledge financial support from Ministerio de Econom?a y Competitividad-FEDER (BFU2016-77691-C2-1-P) and the Generalitat Valenciana (PROMETEO/2016/076).
Funding Information:
D. Fabregat-Safont, J.V. Sancho, F. Hernández and M. Ibáñez acknowledge financial support from the Generalitat Valenciana (PROMETEO/2019/040) and the University Jaume I (UJI-B2018-19). D. Fabregat-Safont acknowledges Ministerio de Educación, Cultura y Deporte in Spain for his predoctoral grant (FPU15/02033). M. Mata-Pesquera acknowledges Ministerio de Educación y Formación Profesional in Spain for her undergraduate research grant (998142). F. Martinez-Garcia and M. Barneo-Muñoz acknowledge financial support from Ministerio de Economía y Competitividad-FEDER (BFU2016-77691-C2-1-P) and the Generalitat Valenciana (PROMETEO/2016/076).
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