Effects of Antidepressants on Neurotransmitters/Receptors*
Amitriptyline | Clomipramine | Desipramine | Doxepin | Imipramine | Nortriptyline | Protriptyline | Trimipramine | Amoxapine | Maprotiline | Bupropion | |
---|---|---|---|---|---|---|---|---|---|---|---|
NE reuptake block | +++ | +++ | +++++ | +++ | +++ | ++++ | +++++ | ++ | ++++ | ++++ | + |
5-HT reuptake block | +++ | ++++ | ++ | ++ | +++ | ++ | ++ | + | ++ | + | – |
DA reuptake block | + | + | + | + | + | + | + | + | + | + | ++ |
5-HT1A blockade | ++ | + | + | ++ | + | ++ | + | + | ++ | – | – |
5-HT2A blockade | +++ | +++ | ++ | +++ | +++ | +++ | +++ | +++ | +++++ | ++ | – |
M1(ACh) blockade | +++ | +++ | ++ | +++ | +++ | ++ | +++ | +++ | ++ | ++ | – |
H1 blockade | ++++ | +++ | ++ | +++++ | +++ | +++ | +++ | +++++ | +++ | ++++ | + |
α1 blockade | +++ | +++ | ++ | +++ | +++ | +++ | ++ | +++ | +++ | +++ | + |
α2 blockade | ++ | + | + | + | + | + | + | + | + | + | – |
D2 blockade | + | ++ | + | + | + | + | + | ++ | ++ | ++ | – |
Selectivity | NE > 5-HT | NE < 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT | NE > 5-HT |
Trazodone | Nefazodone | Venlafaxine(A) | Duloxetine | Citalopram | Escitalopram | Fluoxetine | Fluvoxamine | Paroxetine | Sertraline | Mirtazapine | |
---|---|---|---|---|---|---|---|---|---|---|---|
NE reuptake block | – | ++ | + | ++++ | + | + | ++ | ++ | +++ | ++ | + |
5-HT reuptake block | ++ | ++ | +++ | ++++ | ++++ | ++++ | ++++ | ++++ | +++++ | +++++ | – |
DA reuptake block | – | ++ | + | ++ | – | – | + | – | ++ | +++ | – |
5-HT1A blockade | +++ | +++ | – | + | – | ? | – | – | – | – | +++ |
5-HT2A blockade | +++ | +++ | – | ++ | + | ? | ++ | – | – | + | +++ |
M1(ACh) blockade | – | – | – | + | + | + | ++ | – | ++ | + | ++ |
H1 blockade | ++ | – | – | + | ++ | + | + | – | – | – | ++++ |
α1 blockade | +++ | +++ | – | + | + | + | + | + | + | ++ | ++ |
α2 blockade | ++ | ++ | – | + | – | ? | + | + | + | + | +++ |
D2 blockade | + | ++ | – | – | – | ? | – | – | – | – | + |
Selectivity | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE < 5-HT | NE = 5-HT |
(A) | Desvenlafaxine has similar effects on neurotransmitters as venlafaxine |
Key: Ki (nM) > 10,000 = –; 1000–10,000 = +; 100–1000 = ++; 10–100 = +++; 1–10 = ++++; 0.1–1 = +++++; ? = unknown
See also the National Institute of Mental Health's Psychoactive Drugs Screening Program. Available at http://pdsp.med.unc.edu