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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.

SUBMITTER: Stott LA 

PROVIDER: S-EPMC8219759 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature

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

Stott Lisa A LA   Brighton Cheryl A CA   Brown Jason J   Mould Richard R   Bennett Kirstie A KA   Newman Robert R   Currinn Heather H   Autore Flavia F   Higueruelo Alicia P AP   Tehan Benjamin G BG   MacSweeney Cliona C   O'Brien Michael A MA   Watson Steve P SP  

Heliyon 20210601 6


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. ...[more]

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