Characterisation of AMB-FUBINACA metabolism and CB1-mediated activity of its acid metabolite.

Hunter D. J. Webb, David B. Finlay, Shuli Chen, Andrea J. Vernall, Eric Sparkes, Samuel D. Banister +2 more

Purpose AMB-FUBINACA is a synthetic cannabinoid receptor agonist (SCRA) which is primarily metabolised by hepatic enzymes producing AMB-FUBINACA carboxylic acid. The metabolising enzymes associated with this biotransformation remain unknown. This study aimed to determine if AMB-FUBINACA metabolism could be reduced in the presence of carboxylesterase (CES) inhibitors and recreational drugs commonly consumed with it…

Editorial: Therapeutic potential of the cannabinoid CB2 receptor.

Reem Smoum, Uwe Grether, Meliha Karsak, Andrea J. Vernall, Frank Park, Cecilia J. Hillard +1 more

Cannabinoid Receptor 2 Signalling Bias Elicited by 2,4,6-Trisubstituted 1,3,5-Triazines.

Caitlin R. M. Oyagawa, Sara M. de la Harpe, Yurii Saroz, Michelle Glass, Andrea J. Vernall, Natasha Lillia Grimsey

Cannabinoid receptor 2 (CB2) is predominantly distributed in immune tissues and cells and is a promising therapeutic target for modulating inflammation. In this study we designed and synthesised a series of 2,4,6-trisubstituted 1,3,5-triazines with piperazinylalkyl or 1,2-diethoxyethane (PEG2) chains as CB2 agonists, all of which were predicted to be considerably more polar than typical cannabinoid ligands. In thi…