Table 1 Ligand profiling using MOP phosphorylation assays.
pT370-MOP | pS375-MOP | pT376-MOP | pT379-MOP | |||||
|---|---|---|---|---|---|---|---|---|
Agonist | pEC50 | Emax (% DAMGO) | pEC50 | Emax (% DAMGO) | pEC50 | Emax (% DAMGO) | pEC50 | Emax (% DAMGO) |
DAMGO | 6.1 ± 0.04 | 100 ± 3.2 | 6.0 ± 0.05 | 100 ± 5.3 | 6.0 ± 0.03 | 100 ± 3.5 | 6.0 ± 0.06 | 100 ± 5.9 |
Morphine | 5.6 ± 0.09 | 52.1 ± 3.9 | 5.8 ± 0.07 | 62.3 ± 3.6 | 5.4 ± 0.17 | 19.2 ± 2.8 | 5.5 ± 0.16 | 37.6 ± 5.6 |
Fentanyl | 7.2 ± 0.12 | 88.6 ± 7.4 | 7.0 ± 0.14 | 112.8 ± 13.7 | 6.8 ± 0.11 | 90.8 ± 9.9 | 6.6 ± 0.23 | 112.9 ± 9.1 |
PMA | 7.8 ± 0.12 | 133.9 ± 8.3 | – | – | – | – | – | – |
Antagonist | pIC50 | pIC50 | pIC50 | pIC50 | ||||
Naloxone | 7.3 ± 0.10 | – | 7.1 ± 0.10 | – | 7.4 ± 0.07 | – | 7.4 ± 0.15 | – |
