TABLE 5.
Adenylyl cyclase inhibition, G-protein activation and β arrestin-2 recruitment induced by norepinephrine mediated by α2AR
Data of individual experiments were fit by nonlinear regression to a sigmoidal dose–response relationship against the agonist concentration. The EC50 and Emax values are the mean ± S.E.M. of 3 to 4 experiments performed in triplicate. Emax values are expressed as 1000 × [BRETmax − BRETbasal].
| BRET Assay | Norepinephrine |
|
|---|---|---|
| EC50 (nM) | Emax | |
| Adenylyl cyclase inhibition | 1 ± 0.2 | 76 ± 10 |
| G-protein activation (Gi1) | 12 ± 2 | 24 ± 2 |
| β Arrestin-2 recruitment | 687 ± 247 | 15 ± 1 |