Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

Abstract The identification of cannabinoid ligands Cannabidiol and O-1918 as inverse agonists of the orphan receptor GPR52 is reported. Detailed characterisation of GPR52 pharmacology and modelling of the proposed receptor interaction is described. The identification of a novel and further CNS pharmacology for the polypharmacological agent and marketed drug Cannabidiol is noteworthy. Article type: Research Article Keywords: GPR52, Inverse agonist, Cannabidiol, CBD, O-1918 Authors: Lisa A. Stott, Cheryl A. Brighton, Jason Brown, Richard Mould, Kirstie A. Bennett, Robert Newman, Heather