A new cannabinoid receptor 1 selective agonist evading the 2021 “China ban”: ADB-FUBIATA

Synthetic cannabinoid receptor agonists (SCRAs) carrying new core and linker structures have appeared on the recreational drug market. A very recent example is ADB-FUBIATA, which is structurally closely related to the potent SCRA ADB-FUBICA. ADB-FUBIATA has recently been identified in seized materials in China, Russia, the United States, and also Belgium; its pharmacological characteristics were unknown. The aim of this study was to evaluate the intrinsic cannabinoid receptor (hCB1 and hCB2) activation potential of this previously unknown substance. At CB1, a potency of 635 nM (EC50) was found, with an efficacy (Emax) of 141% relative to the reference compound CP55,940. On the other hand, ADB-FUBIATA had almost no activity at CB2, indicative of a clear CB1 selectivity. This activation pattern differs markedly from that observed for ADB-FUBICA, which was previously found to be potent and efficacious at both cannabinoid receptors. The bioassays were applied to a seized powder containing ADB-FUBIATA, analytically confirmed by HLPC-DAD, gas chromatography coupled to mass spectrometry (GC-MS), liquid chromatography couple to time-of-flight mass spectrometry (LC-QTOF-MS), Fourier transform infrared spectroscopy (FTIR), and nuclear magnetic resonance (NMR). The EC50 and Emax values obtained for this powder were very similar to those of the ADB-FUBIATA analytical standard, suggesting a high purity of the powder, although analytical techniques did reveal that the sample was not entirely pure.

DEVENTER Marie;  VAN UYTFANGHE Katleen;  VINCKIER Inge;  RENIERO Fabiano;  GUILLOU Claude;  STOVE Christophe; 

2022-11-14

WILEY

JRC130512

1942-7603 (online),   

https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/abs/10.1002/dta.3285,    https://publications.jrc.ec.europa.eu/repository/handle/JRC130512,   

10.1002/dta.3285 (online),