Binding affinities of selected compounds at NET, DAT, and SERTa.
| Compound | K i, DAT (nM) | K i, NET (nM) | K i, SERT (nM) | K i, σ1 (nM) |
|---|---|---|---|---|
| GBR12909 | 8.8 ± 3.8b | — | — | — |
| Desipramine | — | 2.5 ± 0.4 | — | — |
| Amitriptyline | — | — | 5.4 ± 0.9 | — |
| 7 | NAc | NA | NA | 1.8 ± 0.2 |
| 18 | 5631d | NA | NA | 0.9 ± 0.1 |
| 22 | >10 000 | 2878 | NA | 2.4 ± 1.2 |
| 24 | 1811 | 1606 | NA | 7.8 ± 3.2 |
| 25 | >10 000 | 1780 | NA | 1.3 ± 0.4 |
| 28 | NA | 7102.5 | NA | 0.2 ± 0.0 |
| 29 | 1518 | 600.5 | NA | 0.4 ± 0.1 |
a
See Experimental section. DAT: dopamine transporter; NET: norepinephrine transporter; SERT: serotonin transporter. Radioligands: DAT: [3H] WIN35428; NET: [3H] nisoxetine; SERT: [3H] citalopram.
b
The Ki values for GBR12909, desipramine, amitriptyline and compound 7 are cited from the literature.27
c
NA: not active, defined as <50% binding in the primary assay at 10 μM. Ki values were determined for those targets where the binding efficacy at 10 μM was greater than 50%.
d
Data are expressed as average of Ki values and each performed from three independent experiments.