| Autor: |
M.H. Deventer, M. Persson, C. Norman, H. Liu, M. Connolly, N.N. Daeid, C. McKenzie, H. Green, C.P. Stove |
| Jazyk: |
angličtina |
| Rok vydání: |
2024 |
| Předmět: |
|
| Zdroj: |
Emerging Trends in Drugs, Addictions, and Health, Vol 4, Iss , Pp 100087- (2024) |
| Druh dokumentu: |
article |
| ISSN: |
2667-1182 |
| DOI: |
10.1016/j.etdah.2023.100087 |
| Popis: |
Introduction: Since the enactment of the Chinese generic ban (2021), the synthetic cannabinoid receptor agonist (SCRA) market has vastly changed and now encompasses unexpected, ban-evading structures such as brominated and tail-less compounds. Methods: Six new SCRAs were functionally characterized at CB1 and CB2 using 2 distinct activity-based assays, monitoring βarr2 recruitment (NanoBiT® assay) and Ca2+ mobilization (AequoScreen® assay). Results: Brominated, tailed SCRAs (ADB-5’Br-BUTINACA, MDMB-5’Br-BUTINACA) showed high efficacy and potency at CB1. Interestingly, switching the bromine for a fluorine (ADB-5’F-BUTINACA) resulted in an even more pronounced CB activity. Tail-less, brominated compounds (ADB-5’Br-INACA, MDMB-5’Br-INACA) retained activity at both receptors, albeit with decreased potency compared to their tailed counterparts, which was confirmed in both assays. Removing the bromine group from the tail-less core resulted in decreased activity (ADB-INACA), evidencing the positive effect of bromine substitution. Conclusions: This study provides essential information for both drug law enforcement agencies and health care workers, as it can be expected that the ever-lasting cat-and-mouse game that describes the SCRA market will carry on, with the surge of new and unexpected substances remaining a great challenge for several fields. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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