Table 3. In vitro efficacy of the compounds in the [35S]GTPγS assay a .
| Compound | MOR |
KOR |
||
| EC50 (nM) | %Emax | EC50 (nM) | %Emax | |
| 9a | 26.42 ± 3.17 | 115.07 ± 7.3 | nd b | nd b |
| 9b | 25.7 ± 1.68 | 120.89 ± 2.55 | nd b | nd b |
| 9c | 4.62 ± 0.28 | 114.36 ± 7.06 | nd b | nd b |
| 9d | 2.83 ± 0.41 | 113.63 ± 4.54 | 58.83 ± 7.49 | 87.88 ± 4.9 |
| 9e | 8.16 ± 2.64 | 114.85 ± 1.26 | nd b | nd b |
| 9f | 7.98 ± 2.35 | 117.16 ± 1.98 | nd b | nd b |
| 2 | 1.38 ± 0.8 | 95.3 ± 0.8 | 36.5 ± 19.2 | 106.3 ± 8.5 |
| DAMGO | 19 ± 7.0 | nd b | nd b | nd b |
| U50,488H | nd b | nd b | 17 ± 6.1 | nd b |
aFunctional properties were studied using agonist-induced stimulation of the [35S]GTPγS binding assay. Potency is represented as EC50 (nM) and efficacy as percent maximal stimulation (%Emax) relative to standard agonist DAMGO (MOR), or U50,488H (KOR) at 100 nM. The protein concentration was 50 μg mL–1 and the incubation time was 90 minutes. All values are expressed as mean ± SEM of three separate assays performed in triplicate.
bNot determined.