Table 2. Antidepressants – inhibition of human serotonin (SERT), norepinephrine (NET) and dopamine (DAT) transporters.
Generic name | Human SERT Kd (nM) | Human NET Kd (nM) | Human DAT Kd (nM) | Selectivity-SERT vs NET |
---|---|---|---|---|
Amitriptyline | 4.3 | 35 | 3250 | 8 |
Amoxepine | 58 | 16 | 4310 | 0.3 |
Bupropion | 9100 | 52,000 | 520 | 5.7 |
Citalopram | 1.2 | 4070 | 28,100 | 3500 |
Clomipramine | 0.3 | 38 | 2190 | 130 |
Desipramine | 17.6 | 0.8 | 3190 | 0.05 |
Dothiepin | 8.6 | 46 | 5310 | 5.3 |
Doxepine | 68 | 29.5 | 12,100 | 0.4 |
Fluoxetine | 0.8 | 240 | 3600 | 300 |
Fluvoxamine | 2.2 | 1300 | 9200 | 580 |
Imipramine | 1.4 | 37 | 8500 | 27 |
Lofepramine | 70 | 5.4 | 18,000 | 0.08 |
Maprotiline | 5800 | 11.1 | 1000 | 0.002 |
Mirtazapine | >100,000 | 4600 | >100,000 | — |
Nefazodone | 200 | 360 | 360 | 1.8 |
Nortriptyline | 18 | 4.4 | 1140 | 0.24 |
Paroxetine | .13 | 40 | 490 | 300 |
Protriptyline | 19.6 | 1.4 | 2100 | 0.07 |
Reboxetine* | 129 | 1.1 | — | 0.008 |
Sertraline | 0.29 | 420 | 25 | 1400 |
Trazodone | 160 | 8500 | 7400 | 53 |
Trimipramine | 149 | 2450 | 780 | 16 |
Venlafaxine | 8.9 | 1060 | 9300 | 120 |
Data from Tatsumi et al. (1997) and *Wong et al. (2000). The results are equilibrium dissociation constants (Kd) in nM, using [3H]-imipramine binding to human SERT, [3H]-nisoxetine binding to human noradrenaline transporter, and 3H-WIN35428 binding to human dopamine transporter (Tatsumi et al., 1997), or for reboxetine *(Wong et al., 2000) [3H]-citalopram binding to human SERT and [3H]-nisoxetine binding to the human NET. The most selective drugs are highlighted in bold in the right hand column.