Table 1. . List of monoamine transporter inhibitors as antidepressant agents.
Inhibitor class | Inhibitor | Year approved | SERT (Ki, nM)† | NET (Ki, nM)† | DAT (Ki, nM)† |
---|---|---|---|---|---|
TCAs | Imipramine | 1951 | 1 | 37 | 8500 |
Trimipramine | 1966 | 149 | 2450 | 1690 | |
Amitriptyline | 1961 | 4 | 35 | 3780 | |
Opipramol | 1961 | N/A‡ | N/A | N/A | |
Desipramine | 1964 | 18 | 1 | 3190 | |
Nortriptyline | 1963 | 18 | 4 | 1140 | |
Protriptyline | 1966 | 20 | 1 | 2100 | |
Dosulepin | 1969 | 9 | 46 | 5310 | |
Butriptyline | 1974 | 1360 | 5100 | 3940 | |
Clomipramine | 1970 | 0.3 | 38 | 2190 | |
Doxepin | 1969 | 68 | 30 | 12,100 | |
Maprotiline | 1974 | 5800 | 11 | 1000 | |
Amoxapine | 1980 | 58 | 16 | 4310 | |
Lofepramine | 1980 | 70 | 5 | 18,000 | |
|
Amineptine |
1983 |
N/A |
N/A |
N/A |
SSRI | Zimelidine | 1982 | 152 | 9400 | 11,700 |
Fluoxetine | 1987 | 1 | 240 | 3600 | |
Paroxetine | 1992 | 0.1 | 40 | 490 | |
Fluvoxamine | 1994 | 2 | 1300 | 9200 | |
Citalopram | 1989 | 1 | 4070 | 28,100 | |
Sertraline | 1991 | 0.3 | 420 | 25 | |
|
Escitalopram |
2001 |
1 |
>10000 |
>10,000 |
SNRI | Sibutramine | 1997 | N/A | N/A | N/A |
Venlafaxine | 1993 | 9 | 1060 | 9300 | |
Milnacipran | 2009 | 420 | 77 | 6100 | |
Duloxetine | 2004 | 1 | 8 | 240 | |
Desvenlafaxine | 2008 | 40 | 558 | >100,000 | |
|
Levomilnacipran§ |
2013 |
11 |
92 |
>10,000 |
NRI | Viloxazine | 1977 | 17,300 | 155 | >100,000 |
Mirtazapine | 1994 | >100,000 | 4600 | >100,000 | |
Atomoxetine | 2002 | 152 | 5 | 658 | |
|
Reboxetine |
1999 |
242 |
3 |
>100,000 |
DRI |
Bupropion |
1985 |
9100 |
52,000 |
520 |
NRI/DRI |
Nomifensine |
1977 |
1010 |
16 |
562 |
SMS¶ | Trazodone | 1981 | 160 | 8500 | 7400 |
Nefazodone | 1994 | 200 | 360 | 360 | |
Vilazodone# | 2011 | 0.1 | 56 | 37 | |
Vortioxetine†† | 2013 | 1.6 | 113 | >1000 |
‡N/A, no data available for human-cloned receptors.
§Activity values taken from [62].
¶Serotonin modulator and stimulator.
#Activity values taken from [63].
††Activity values taken from [64].
DAT: Dopamine transporter; DRI: Dopamine reuptake inhibitor; NET: Norepinephrine transporter; NRI: Norepinephrine reuptake inhibitor; SERT: Serotonin transporter; SNRI: Serotonin/norepinephrine reuptake inhibitor; SRS: Serotonin modulator and stimulator; SSRI: Selective serotonin reuptake inhibitor; TCA: Tricyclic antidepressant.