TABLE 1.
In vitro binding affinities and functional activities of NOP ligands
Binding was conducted as described in Materials and Methods. Values shown represent mean ± S.D.
| Receptor Binding Ki |
[35S]GTPγS NOP |
[35S]GTPγS MOP |
|||||
|---|---|---|---|---|---|---|---|
| NOP | MOP | KOP | EC50 | Stimulation | EC50 | Stimulation | |
| nM | nM | % | nM | % | |||
| N/OFQ | 0.2 ± 0.04 | 133 ± 30 | 247 ± 3.4 | 4.0 ± 0.1 | 100 | >10,000 | |
| Morphine | >10,000 | 1.1 ± 0.1 | 46.9 ± 14.5 | 0 | 5.2 ± 1.6 | 93 ± 2.8 | |
| SR14150 | 1.39 ± 0.42 | 29.9 ± 2.1 | 42.7 ± 1.0 | 20.8 ± 3.1 | 54.2 ± 10.9 | 99 ± 12 | 23.4 ± 3.2 |
| SR16507 | 5.22 ± 0.65 | 1.07 ± 0.17 | 82.4 ± 16.4 | 8.5 ± 0.8 | 95 ± 12 | 5.2 ± 1.6 | 47 ± 1.5 |
| SR16835 | 11.4 ± 0.9 | 79.9 ± 3.9 | 681.3 ± 61.6 | 46.1 ± 20.5 | 106.6 ± 7.4 | 129 ± 48 | 18 ± 1.6 |