Table 2.
Compd | Structure | R | R’ | SERT Ki±SEM (nM) |
NET Ki±SEM (nM) |
Ki (NET)/Ki (SERT) |
---|---|---|---|---|---|---|
24 | B | CN | Br | 50.9±3.89 | 17% b | >10,000 |
25 | A | CN | Br | 11.4±0.74 | 45% b | |
26 | A | CN | 38.0±4.21 | 44% b | >10,000 | |
27 | A | CN | 51.5±6.63 | 2800±353 | 54 | |
28 | A | CN | 125±15.2 | 7020±581 | 56 | |
37 | C | _ | _ | 681±88.2 | 4970±738 | 7.3 |
These novel analogues were assessed by radioligand binding displacement of [3H]1 (for SERT) and [3H]nisoxetine (for NET) in rat brain stem and frontal cortex, respectively.35
% Displacement at 10 µM.