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

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 f...

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Detalles Bibliográficos
Autores principales: Stott, Lisa A., Brighton, Cheryl A., Brown, Jason, Mould, Richard, Bennett, Kirstie A., Newman, Robert, Currinn, Heather, Autore, Flavia, Higueruelo, Alicia P., Tehan, Benjamin G., MacSweeney, Cliona, O'Brien, Michael A., Watson, Steve P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8219759/
https://www.ncbi.nlm.nih.gov/pubmed/34189291
http://dx.doi.org/10.1016/j.heliyon.2021.e07201
Descripción
Sumario: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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