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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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
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author 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.
author_facet 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.
author_sort Stott, Lisa A.
collection PubMed
description 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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spelling pubmed-82197592021-06-28 Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918 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. Heliyon Research Article 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. Elsevier 2021-06-01 /pmc/articles/PMC8219759/ /pubmed/34189291 http://dx.doi.org/10.1016/j.heliyon.2021.e07201 Text en Crown Copyright © 2021 Published by Elsevier Ltd. https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Research Article
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.
Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918
title Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918
title_full Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918
title_fullStr Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918
title_full_unstemmed Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918
title_short Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918
title_sort characterisation of inverse agonism of the orphan-g protein-coupled receptor gpr52 by cannabinoid ligands cannabidiol and o-1918
topic Research Article
url 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
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