| Autor: |
Jara, Bouma, Marjolein, Soethoudt, Noortje, van Gils, Lizi, Xia, Mario, van der Stelt, Laura H, Heitman |
| Jazyk: |
angličtina |
| Rok vydání: |
2023 |
| Předmět: |
|
| Zdroj: |
Methods in molecular biology (Clifton, N.J.). 2576:189-199 |
| ISSN: |
1064-3745 |
| Popis: |
Cannabinoid receptor 1 (CB1R) and cannabinoid receptor 2 (CB2R) are G protein-coupled receptors (GPCRs) that activate a variety of pathways upon activation by (partial) agonists including the G protein pathway and the recruitment of β-arrestins. Differences in the activation level of these pathways lead to biased signaling. Here, we describe a detailed protocol to characterize the potency and efficacy of ligands to induce or inhibit β-arrestin recruitment to the human CB1R and CB2R using the PathHunter® assay. This is a cellular assay that uses a β-galactosidase complementation system which has a chemiluminescent read-out and can be performed in 384-well plates. We have successfully used this assay to characterize a set of reference ligands (both agonists, antagonists, and an inverse agonist) on human CB1R and CB2R, of which some examples will be presented here. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
