Table 1. Δ6-Gαqi4myr-mediated Ca2+ release of HEK-293 cells stably expressing opioid receptors.
| Ca2+ release | 6′-GNTI | U69,593 | DPDPE | DAMGO |
|---|---|---|---|---|
| EC50, nM | ||||
| KOP | 224.4 ± 14.2 | 0.83 ± 0.07 | >1,000 | >1,000 |
| DOP | >1,000 | >1,000 | 22.1 ± 1.3 | >1,000 |
| MOP | >1,000 | >1,000 | >1,000 | 6.5 ± 2.2 |
| KOP/DOP | 39.8 ± 3.0 | 0.82 ± 2.5 | 53.1 ± 2.2 | >1,000 |
| KOP/MOP | 112.5 ± 3.1 | 0.34 ± 3.2 | >1,000 | 20.9 ± 1.8 |
| DOP/MOP | >1,000 | >1,000 | 43.2 ± 6.7 | 5.6 ± 2.6 |
| Emax, RLU | ||||
| KOP | 367.9 ± 165.7 | 518.8 ± 299.8 | — | — |
| DOP | — | — | 295.6 ± 65.4 | — |
| MOP | — | — | — | 689.4 ± 314.0 |
| KOP/DOP | 404.3 ± 140.2 | 570.7 ± 156.6 | 441.2 ± 33.0 | — |
| KOP/MOP | 272.2 ± 137.2 | 458.1 ± 206.8 | — | 536.2 ± 270.9 |
| DOP/MOP | — | — | 604.8 ± 209.1 | 531.7 ± 210.9 |
Data are mean ± SEM (n = 3-5). RLU, relative luciferase units; DAMGO, [d-Ala2-MePhe4-Gly5-ol]; —, not applicable.