Table 2.

In vitro affinities versus in vivo occupancy rates at typical clinical dosing for antidepressants

Antidepressant	In vitro Ki, nM	In vivo brain occupancy, %*
Moclobemide26,39	6–14 ×103 (MAO-A)	74
St. John’s wort (Hypericin perforatum)40	> 200 ×103 (MAO-A)	< 10
Buproprion10–12,41,42	630 (DAT)	14
Escitalopram43	1.1 (5-HTT)	82
Citalopram7,9,42	20 (5-HTT)	81
Sertraline7,42	39–65 (5-HTT)	85
Fluoxetine7,42,43	11–18 (5-HTT)	76
Paroxetine6,7,9	8 (5-HTT)	85
Duloxetine44,45	0.8 (5-HTT)	82
Venlaflaxine7,45	10 (5-HTT)	84

5-HTT = serotonin transporter; DAT = dopamine transporter; Ki = equilibrium dissociation constant; MAO-A = monoamine oxidase A.

^*Occupancy at typical clinical dosing in the primary region of interest.