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cc by (c) Sánchez Fernández, Nuria et al., 2024
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/219512

Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells

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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.

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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. Cannabidiol negatively modulates adenosine A2A receptor functioning in living cells. _Acta Neuropsychiatrica_. 2024. Vol. 36, núm. 5, pàgs. 320-324. [consulta: 25 de febrer de 2026]. ISSN: 0924-2708. [Disponible a: https://hdl.handle.net/2445/219512]

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