Pharmacological characterization of MOM-Sal B
Competitive Inhibition of [3H]Diprenorphine Binding | [35S]GTPγS Binding | Internalization of FLAG-hKOPR | Down-Regulation of FLAG-hKOPR | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Ki | EC50 | Emax* | EC50 | Emax* | EC50 | Emax* | ||||
| nM | nM | nM | nM | |||||||
| U50,488H | 1.4 ± 0.3 | 3.4 ± 0.5 | 100 | 97.1 ± 19.2 | 100 | 125.1 ± 42.0 | 100 | |||
| Sal A | 1.3 ± 0.5 | 4.5 ± 1.2 | 100.2 ± 5.1 | 522.2 ± 45.1 | 96.1 ± 1.5 | 142.1 ± 10.7 | 94.3 ± 2.8 | |||
| MOM-Sal B | 0.4 ± 0.02 | 0.6 ± 0.2 | 97.8 ± 6.4 | 7.4 ± 0.5 | 109.2 ± 4.2 | 6.3 ± 1.2 | 89.0 ± 3.9 | |||
↵* Efficacy determined as the percentage of maximal response produced by U50,488H.