Table 3. Stimulation of [35S]GTPγS Bindinga.
μ receptor |
δ receptor |
κ receptor |
||||
---|---|---|---|---|---|---|
compd | EC50 (nM) | % stimb | EC50 (nM) | % stimc | EC50 (nM) | % stimd |
17 | 0.69 ± 0.10 | 34.7 ± 6.6 | 0.69 ± 0.29 | 26.1 ± 3.0 | 1.28 ± 0.35 | 28.2 ± 1.0 |
18 | 1.06 ± 0.28 | 24.2 ± 3.0 | 4.24 ± 0.47 | 34.7 ± 0.6 | 11.0 ± 1.4 | 30.4 ± 3.3 |
morphine | 15.6 ± 0.5 | 93 ± 2.8 | 316 ± 5 | 103 ± 7 | 484 ± 213 | 62 ± 7 |
Membranes from CHO cells stably transfected with human μ, δ, or κ opioid receptors were incubated with varying concentrations of the compounds.
Compared to DAMGO.
Compared to DPDPE.
Compared to U69,593. Data represent mean ± SEM.