Table 2.
Effect of specific substructural modifications on selectivity for S1R over S2R.
| Compound | Substructural feature | S1R affinity (Ki, nM) | S2R affinity (Ki, nM) | S2R/S1R ration (Ki S2R / Ki S1R) |
|---|---|---|---|---|
| Carbetapentane |
|
19.8 ± 2.3 | 55.7 ± 3.8 | 3 |
| Oxeladin |
|
25 ± 4.3 | 148 ± 64 | 6 |
| Butamirate |
|
17.2 ± 1.7 | 214 ± 41 | 10 |