TABLE 1.
Binding affinity and in vitro functional activity at NOP and MOP receptors
Binding was conducted as described in Materials and Methods. Values shown represent mean ± S.D. of at least two experiments conducted in triplicate.
| Receptor Binding Ki |
[35S]GTPγS NOPr |
[35S]GTPγS MOPr |
||||
|---|---|---|---|---|---|---|
| NOPr | MOPr | EC50 | Stim | EC50 | Stim | |
| nM | nM | % | nM | % | ||
| SR 16435 | 8.0 ± 7.5 | 2.7 ± 0.5 | 28.7 ± 0.6 | 45.0 ± 5 | 29.5 ± 10.3 | 30 ± 0.2 |
| SR16507 | 5.22 ± 0.65 | 1.07 ± 0.17 | 8.5 ± 0.8 | 95 ± 12 | 5.2 ± 1.6 | 47 ± 1.5 |
| Buprenorphine | 77.4 ± 16 | 1.5 ± 0.8 | 251.2 ± 94.0 | 15.5 ± 5.8 | 10.2 ± 2.21 | 28.7 ± 1.05 |
| Morphine | >10,000 | 1.1 ± 0.1 | 0 | 15.6 ± 0.5 | 93 ± 2.8 | |
| Pentazocine | >10,000 | 3.9 ± 0.7 | 0 | 39.5 ± 0.25 | 20.2 ± 3.4 | |
| SB-612111 | 1.42 ± 0.12 | 674 ± 43.9 | 0 | 0 | ||
NOPr, NOP receptor; MOPr, MOP receptor; Stim, stimulation.