Table 1.
Heat-map of average antidepressant drug concentrations resulting in 50% inhibition (IC50) of 5-HT uptake by MVM (SERT-mediated) and BM (OCT3-mediated). 5-HT transport inhibition clearly occurs at clinically relevant concentrations, according to published Cmax [48,49], Ca [49,50] and F/M ratio [51] values. The red color intensity indicates the inhibitory potency of antidepressants based on the obtained IC50 values.
| Antidepressant | nM | F/M Ratio |
|||||
|---|---|---|---|---|---|---|---|
| IC50 | IC50 | Ca | Cmax | Ca;fetal | |||
| MVM | BM | ||||||
| Stronger inhibitor | Paroxetine | 10.09 | 4.39 | 455 | 1000 | 209 | 0.46 |
| Citalopram | 16.52 | 15.07 | 216 | 1200 | 147 | 0.68 | |
| Fluvoxamine | 19.95 | 15.21 | 446 | 1300 | 348 | 0.78 | |
| Weaker inhibitor | Fluoxetine | 29.99 | 25.18 | 557 | 1900 | 368 | 0.66 |
| Sertraline | 25.18 | 34.43 | 104 | 1300 | 53 | 0.51 | |
| Venlafaxine | 32.07 | 30.76 | 225 | 1400 | 162 | 0.72 | |
Abbreviations: Cmax—maximum steady-state plasma concentration; Ca—average maternal plasma concentration; Ca;fetal—average fetal plasma concentration; F/M ratio—antidepressant’s fetal-to-maternal concentration ratio.