Table 4.
Affinity fentanyl-based MOR/D2R MTAs. Data taken from [77].
| Compound | Ar (Refer to Figure 6) |
n | D2R Receptor Binding, [Ki (nM)] 1 |
|---|---|---|---|
| 5.3 | Ph | 2 | 869 |
| 5.4 | 2-OMe-Ph | 2 | 800 |
| 5.5 | 2,3-Cl2-Ph | 2 | 594 |
| 5.6 | Ph | 3 | 1357 |
| 5.7 | 2-OMe-Ph | 3 | 7992 |
| 5.8 | 3-OMe-Ph | 3 | n/d 2 |
| 5.9 | 2,3-Cl2-Ph | 3 | 6956 |
| 5.10 | Ph | 4 | 7083 |
| 5.11 | 2-OMe-Ph | 4 | 4436 |
| 5.12 | 2,3-Cl2-Ph | 4 | 2376 |
| 5.13 | Ph | 5 | 8105 |
| 5.14 | 2-OMe-Ph | 5 | 3778 |
| 5.15 | 2,3-Cl2-Ph | 5 | 1500 |
| 5.16 | Ph | 6 | 1853 |
| 5.17 | 2-OMe-Ph | 6 | 5454 |
| 5.18 | 2,3-Cl2-Ph | 6 | 5326 |
1 Ki, inhibition constant, competitive radioligand binding assay with 0.2 nM [3H]-spiperone as radioligand, in preparations of rat caudate nuclei synaptosomal membranes, 2 n/d—not determined.