PubMed: Cannabidiol negatively modulates adenosine A<sub>2A</sub> receptor functioning in living cells
Acta Neuropsychiatr. 2023 Aug 22:1-14. doi: 10.1017/neu.2023.30. Online ahead of print.
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 NanoBiTTM 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.
https://pubmed.ncbi.nlm.nih.gov/37605951/?utm_source=Chrome&utm_medium=rss&utm_campaign=pubmed-2&utm_content=1NqsX9BbHlDygQ8TcgAlJilHgPpiuKQtyIr–a3-xbLzPoB9xM&fc=20220928170152&ff=20230822190613&v=2.17.9.post6+86293ac August 22, 2023 10:00 am