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

Autor: Lisa A. Stott, Cheryl A. Brighton, Jason Brown, Richard Mould, Kirstie A. Bennett, Robert Newman, Heather Currinn, Flavia Autore, Alicia P. Higueruelo, Benjamin G. Tehan, Cliona MacSweeney, Michael A. O'Brien, Steve P. Watson
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Zdroj: Heliyon, Vol 7, Iss 6, Pp e07201- (2021)
Druh dokumentu: article
ISSN: 2405-8440
DOI: 10.1016/j.heliyon.2021.e07201
Popis: 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.
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