Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells
Objectives: Cannabidiol (CBD) is a phytocannabinoid with great potential in clinical applications. The mechanism(s) of action of CBD require further investigation. Previous studies suggested that adenosine A2A receptors (A2ARs) could play a role in CBD-induced effects. Here, we evaluated the ability...
| Autores: | ; ; ; ; ; ; ; ; |
|---|---|
| Tipo de documento: | Artigo |
| Estado: | Published version |
| Data de publicação: | 2024 |
| País: | España |
| Recursos: | Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
| Repositório: | Recercat. Dipósit de la Recerca de Catalunya |
| OAI Identifier: | oai:recercat.cat:2445/219512 |
| Acesso em linha: | https://hdl.handle.net/2445/219512 |
| Nível de acesso: | Acesso aberto |
| Palavra-chave: | Cànnabis Adenosina Cèl·lules epitelials Cannabis Adenosine Epithelial cells |
| _version_ | 1878738202257260544 |
|---|---|
| author | Sánchez Fernández, Nuria |
| author2 | Gómez Acero, Laura Sarasola, Laura I. Argerich Bergadà, Josep Chevigné, Andy Jacobson, Kenneth A. Ciruela Alférez, Francisco Fernández Dueñas, Víctor Aso Pérez, Ester |
| author2_role | author author author author author author author author |
| author_browse | Argerich Bergadà, Josep Aso Pérez, Ester Chevigné, Andy Ciruela Alférez, Francisco Fernández Dueñas, Víctor Gómez Acero, Laura Jacobson, Kenneth A. Sarasola, Laura I. Sánchez Fernández, Nuria |
| author_facet | Sánchez Fernández, Nuria Gómez Acero, Laura Sarasola, Laura I. Argerich Bergadà, Josep Chevigné, Andy Jacobson, Kenneth A. Ciruela Alférez, Francisco Fernández Dueñas, Víctor Aso Pérez, Ester |
| author_role | author |
| collection | Recercat. Dipósit de la Recerca de Catalunya |
| description | Objectives: Cannabidiol (CBD) is a phytocannabinoid with great potential in clinical applications. The mechanism(s) of action of CBD require further investigation. Previous studies suggested that adenosine A2A receptors (A2ARs) could play a role in CBD-induced effects. Here, we evaluated the ability of CBD to modify the function of A2AR. Methods: We used HEK-293T cells transfected with the cDNA encoding the human A2AR and Gαs protein, both modified to perform bioluminescence-based assays. We first assessed the effect of CBD on A2AR ligand binding using an A2AR NanoLuciferase sensor. Next, we evaluated whether CBD modified A2AR coupling to mini-Gαs proteins using the NanoBiT™ assay. Finally, we further assessed CBD effects on A2AR intrinsic activity by recording agonist-induced cAMP accumulation. Results: CBD did not bind orthosterically to A2AR but reduced the coupling of A2AR to Gαs protein and the subsequent generation of cAMP. Conclusion: CBD negatively modulates A2AR functioning. |
| eu_rights_str_mv | openAccess |
| format | article |
| id | ES_ab28ae3a746c253564dca01e64c64e5f |
| institution | Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
| instname_str | Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
| network_acronym_str | ES |
| network_name_str | España |
| oai_identifier_str | oai:recercat.cat:2445/219512 |
| publishDate | 2024 |
| publishDateSort | 2024 |
| publisher | Cambridge University Press (CUP) |
| publisherStr | Cambridge University Press (CUP) |
| reponame_str | Recercat. Dipósit de la Recerca de Catalunya |
| spelling | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells Sánchez Fernández, Nuria Gómez Acero, Laura Sarasola, Laura I. Argerich Bergadà, Josep Chevigné, Andy Jacobson, Kenneth A. Ciruela Alférez, Francisco Fernández Dueñas, Víctor Aso Pérez, Ester Cànnabis Adenosina Cèl·lules epitelials Cannabis Adenosine Epithelial cells Objectives: Cannabidiol (CBD) is a phytocannabinoid with great potential in clinical applications. The mechanism(s) of action of CBD require further investigation. Previous studies suggested that adenosine A2A receptors (A2ARs) could play a role in CBD-induced effects. Here, we evaluated the ability of CBD to modify the function of A2AR. Methods: We used HEK-293T cells transfected with the cDNA encoding the human A2AR and Gαs protein, both modified to perform bioluminescence-based assays. We first assessed the effect of CBD on A2AR ligand binding using an A2AR NanoLuciferase sensor. Next, we evaluated whether CBD modified A2AR coupling to mini-Gαs proteins using the NanoBiT™ assay. Finally, we further assessed CBD effects on A2AR intrinsic activity by recording agonist-induced cAMP accumulation. Results: CBD did not bind orthosterically to A2AR but reduced the coupling of A2AR to Gαs protein and the subsequent generation of cAMP. Conclusion: CBD negatively modulates A2AR functioning. Cambridge University Press (CUP) https://hdl.handle.net/2445/219512 |
| spellingShingle | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells Sánchez Fernández, Nuria Cànnabis Adenosina Cèl·lules epitelials Cannabis Adenosine Epithelial cells |
| status_str | publishedVersion |
| title | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells |
| title_full | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells |
| title_fullStr | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells |
| title_full_unstemmed | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells |
| title_short | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells |
| title_sort | Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells |
| topic | Cànnabis Adenosina Cèl·lules epitelials Cannabis Adenosine Epithelial cells |
| topic_facet | Cànnabis Adenosina Cèl·lules epitelials Cannabis Adenosine Epithelial cells |
| url | https://hdl.handle.net/2445/219512 |