Table 2.
Functional activity of Dezocine at human κ-, rat μ, or rat δ-opioid receptors.
| Compounds | Agonist activity | Antagonist activity | |||||||
|---|---|---|---|---|---|---|---|---|---|
| MOR | KOR | DOR | MOR | KOR | DOR | ||||
| EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) | Ke (nM) | Ke (nM) | Ke (nM) | |
| DAMGO | 16.1 ± 0.3 | 240.7 ± 33.8 | c | c | c | c | c | c | c |
| U50,488 H | c | c | 5.6 ± 1.2 | 198.9 ± 7.5 | c | c | c | c | c |
| DPDPE | c | c | c | c | 1.4 ± 0.2 | 231.3 ± 7.1 | c | c | c |
| Dezocine | b | 45.8 ± 1.1d | b | 33.6 ± 2.4d | b | 26.1 ± 1.0d | 10.4 ± 4.9 | 324.1 ± 23.6 | a |
Membranes were incubated with varying concentrations of ligands in the presence of 0.1 nM [35S]GTPγS. Data are expressed as the mean ± SEM for at least three independent experiments performed in triplicate.
aNot tested because of low affinity at DOR. bLow stimulation at 10 μM. cNot applicable. dThe agonist efficacy at 10 μM.