Skip to main content
. 2015 Nov;7(17):2385–2405. doi: 10.4155/fmc.15.134

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

Activity values taken from [60] and [61] unless otherwise specified.

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.