Agonistic activities of TRK-130, DAMGO, DPDPE, U-69593, morphine, and buprenorphine on forskolin-stimulated cAMP accumulation in human MOR-, DOR-, and KOR-expressed cells
EC50 values are defined as the concentration of a compound required for the half-maximum inhibition and expressed as means with 95% confidence intervals in parentheses. Emax values are expressed as means ± S.E.M. of six wells obtained from three independent experiments.
| Compound | MOR | DOR | KOR | |||
|---|---|---|---|---|---|---|
| EC50 | Emax | EC50 | Emax | EC50 | Emax | |
| nM | % | nM | % | nM | % | |
| TRK-130 | 2.39 (1.85–3.09) | 66.1 ± 3.9a,b,c | 26.1 (22.4–30.5) | 71.0 ± 1.9d,e | 9.51 (8.40-10.8) | 62.6 ± 1.3d,e |
| Morphine | 19.9 (18.4–21.5) | 100.0 ± 1.0 | N.D. | N.D. | N.D. | N.D. |
| Buprenorphine | 4.49 (4.11–4.91) | 90.8 ± 1.4a,b | 8.00 (6.59–9.68) | 62.2 ± 2.4d | 2.08 (1.53–2.68) | 20.5 ± 0.7d |
| DAMGO | 2.07 (1.92–2.23) | 100.0 ± 0.9 | ||||
| DPDPE | 0.527 (0.456–0.608) | 100.0 ± 0.7 | ||||
| U-69593 | 1.64 (1.55–1.73) | 100.0 ± 0.4 | ||||
N.D., not determined.
↵a P < 0.05 versus the corresponding full agonist by Steel-Dwass test.
↵b P < 0.05 versus morphine by Steel-Dwass test.
↵c P < 0.05 versus buprenorphine by Steel-Dwass test.
↵d P < 0.05 versus the corresponding full agonist by Tukey test.
↵e P < 0.05 versus buprenorphine by Tukey test.