Table 2.
Opioid receptor efficacy of peptidomimetics
| EC50(nM) | % Stimulation | |||||
|---|---|---|---|---|---|---|
| Compound | MOR | DOR | KOR | MOR | DOR | KOR |
| 1 (4R) | 1.6 ± 0.3 | 110 ± 6 | 540 ± 72 | 81 ± 2 | 16 ± 2 | 22 ± 2 |
| 15a | 1.1 ± 0.3 | dns | dns | 45 ± 5 | dns | dns |
| 15b | 0.84 ± 0.35 | 69 ± 35 | dns | 93 ± 5 | 15 ± 1 | dns |
| 15c | 0.53 ± 0.08 | dns | dns | 96 ± 3 | dns | dns |
| 15d | 0.24 ± 0.03 | dns | 68 ± 15 | 86 ± 1 | dns | 38 ± 2 |
| Morphine * | 194 ± 21 | nt | nt | 57 ± 5 | ||
Efficacy data were obtained using agonist induced stimulation of [35S] GTPγS binding assay. Efficacy is represented as EC50 (nM) and percent maximal stimulation relative to standard agonists DAMGO (MOR), DPDPE (DOR) or U69,593 (KOR) at 10μM concentrations. All values are expressed as mean ± SEM of three separate assays performed in duplicate.
dns: does not stimulate; nt: not tested.
*
From 7.