Table 2.
Opioid receptor efficacy for analogues 10a-o.a
| EC50 (nM) | % stimulation | |||||
|---|---|---|---|---|---|---|
| Compound | MOR | DOR | KOR | MOR | DOR | KOR |
| (Fig 1a) | 1.6±0.3b | 110±6b | 540±72b | 81±2b | 16±2b | 22±2b |
| 10a | 93±20 | dns | dns | 37±7 | dns | dns |
| 10b | 9±1 | dns | dns | 73±8 | dns | dns |
| 10c | 25±11 | dns | dns | 52±2 | dns | dns |
| 10d | 60±2 | dns | dns | 82±2 | dns | dns |
| 10e | dns | dns | dns | dns | dns | dns |
| 10f | 72±24 | dns | > 1000 | 18±2 | dns | > 40 |
| 10g | 23±13 | dns | dns | 34±6 | dns | dns |
| 10h | 2.2±0.9 | dns | dns | 84±6 | dns | dns |
| 10i | 14±3 | dns | dns | 36±3 | dns | dns |
| 10j | 3±1 | dns | 15±9 | 96±4 | dns | 14±2 |
| 10k | 0.4±0.1 | dns | 90±65 | 105±6 | dns | 25±4 |
| 10l | 2.0±0.5 | dns | 600±400 | 56±2 | dns | 14±1 |
| 10m | 6±2 | dns | 160±36 | 91±8 | dns | 46±5 |
| 10n | 0.9±0.4 | dns | 400±130 | 118±5 | dns | 32±1 |
| 10o | 40±20 | dns | > 2000 | 72±3 | dns | > 20 |
a
Efficacy data were obtained using agonist induced stimulation of [35S]GTPγS binding in membrane preparations expressing either MOR, DOR or KOR. Potency is represented as EC50 (nM) and efficacy as percent maximal stimulation relative to standard agonist DAMGO (MOR), DPDPE (DOR), or U69,593 (KOR) at 10 μM. All values are expressed as the mean ± SEM of three separate assays performed in duplicate. dns: does not stimulate.
b
Data from Ref. 17