Table 3.
Neurokinin receptor NK2 and NK3 ligand binding assay.
| Compounds | IC50 [nM] ± SEM | Ki [nM] ± SEM | |
|---|---|---|---|
| References | [Nle10]-NKA(4-10) | 2.1 | 1.1 |
| SB 222200 | 10 | 5.7 | |
| NK2 pharmacophores | SBL-OPNK-1 | 33.6 ± 11.9 a | 18.3 ± 13.0 |
| SBL-OPNK-2 | n.c. a | n.c. | |
| NK3 pharmacophore | SBL-OPNK-3 | 20.3 ± 7.2 b | 11.0 ± 7.8 |
| Hybrids | SBL-OPNK-5 | 3.0 ± 1.0 a | 1.6 ± 1.1 |
| SBL-OPNK-7 | 0.63 ± 0.22 a | 0.34 ± 0.24 | |
| SBL-OPNK-9 | 6.7 ± 2.4 b | 3.6 ± 2.5 | |
a Determined on the NK2 receptor. b Determined on the NK3 receptor. n.c., not calculated: concentration–response curve showed less than 25% inhibitory binding at the highest validated test concentrations.