Table 4.
35S-GTPγS binding parameters in mouse brainstem membranes
| Agonist | Stimulation | + 1µM DAMGO or SR-14968 | ||||
| Fig. 4 | EC50, nM | % Emax* | n | IC50, nM | % Emax* | n |
| A–E. DAMGO | 240 (188 to 305) | 100% | 30 | – | – | |
| A Sufentanil | 0.48 (0.10 to 2.24) | 31 (26 to 37) | 5 | 6.0 (1.1 to 40) | 32 (17 to 43) | 5 |
| B Oliceridine | NC | [10 ± 5] | 7 | 72 (30 to 169) | 12 (0 to 25) | 5 |
| C SR-11501 | 103 (25 to 449) | 42 (34 to 52) | 5 | 91 (11 to 811) | 45 (34 to 54) | 5 |
| D SR-17018 | 124 (52 to 294) | 48 (42 to 56) | 9 | NC | [78 ± 2] | 4 |
| E SR-15099 | 101 (26 to 341) | 29 (22 to 37) | 5 | NC | [75 ± 11] | 3 |
| EC50, nM | % Emax† | n | IC50, nM | % Emax† | n | |
| F SR-14968 | 88 (48 to 159) | 100% | 4 | – | – | |
| G SR-17018 | 132 (35 to 479) | 42 (32 to 53) | 4 | NC | [36 ± 6] | 4 |
*Percent Emax of DAMGO; bottom, shaded.
†Percent Emax of SR-14968; the means are presented with 95% CI, the number of mice is indicated (n), and DAMGO was included in every experiment. Competition parameters were derived by constraining the top to the average 1 µM DAMGO (or SR-14968) response obtained in each experiment. Bracketed [Emax] values represent the percent stimulation at the highest concentration tested for curves that did not converge (NC).