Table 2.
Agonist-stimulated 35S-GTPγS binding in the presence of increasing naloxone
| Fig. 3 A–C | DAMGO | SR-17018 | SR-14968 | ||||
| 35S-GTPγS | |||||||
| [Naloxone] | EC50, nM | %Emax | EC50, nM | %Emax | EC50, nM | %Emax | αβ |
| None | 17 (14 to 20) | 100 | 62 (44 to 87) | 59 (55 to 62) | 3.9 (3.1 to 5.0) | 99 (96 to 103) | 0.0029 |
| 1 nM | 36 (32 to 42) | shared | 217 (149 to 317) | shared | 7.2 (5.4 to 9.6) | 99 (95 to 103) | |
| 10 nM | 166 (148 to 186) | shared | 2085 (1397 to 3058) | shared | 27 (20 to 34) | 92 (88 to 96) | |
| 100 nM | 1455 (1211 to 1749) | shared | 12070(8134 to 18660) | shared | 168 (123 to 227) | 70 (65 to 75) | |
Mean parameters with 95% CI are shown, n = 3, see Fig. 3. αβ is provided for the fit of the allosteric operational model for SR-14968.