Table 2. FDA-approved antidepressants inhibit sphere formation by HCC1954 breast tumor cells.
Drug | Approved Drug Class | Molecular Target(s) | IC50 |
---|---|---|---|
Clomipramine | Tricyclic Antidepressant | SERT, 5-HT2A, 2C, 3, 6, 7 | 1.9 |
Doxepin | Tricyclic Antidepressant | SERT, 5-HT1A, 2A, 2C, 6 | 4.1 |
Latrepirdine | Tricyclic Antihistamine | 5-HT2C, 5A, 6 | 4.2 |
Cyproheptadine | Tricyclic Antihistamine | 5-HT1A, 2A, 2B, 2C, 3, 6, 7 | 6.0 |
Mianserin | Tetracyclic Antidepressant | 5-HT1F, 2A, 2B, 2C, 6, 7 | 12.5 |
Ziprasidone | Atypical Antipsychotic | SERT, 5-HT1A, 1B, 1D, 2A, 2C, 6, 7 | 0.8 |
Asenapine | Atypical Antipsychotic | 5-HT1A, 1B, 2A, 2B, 2C, 5A, 6, 7 | 7.5 |
Vortioxetine | Selective Serotonin Reuptake Inhibitor | SERT, 5-HT1A, 1B, 1D, 3A, 7 | 1.1 |
Vilazodone | Selective Serotonin Reuptake Inhibitor | SERT, 5-HT1A | 1.6 |
Fluoxetine | Selective Serotonin Reuptake Inhibitor | SERT, 5-HT2A, 2C | 3.4 |
Paroxetine | Selective Serotonin Reuptake Inhibitor | SERT | 2.7 |
Sertraline | Selective Serotonin Reuptake Inhibitor | SERT | 1.1 |
HCC1954 tumorspheres were grown in the presence of different FDA-approved serotonergic antidepressants and their effect on sphere formation monitored. All the antidepressants reduced sphere formation in a dose-dependent fashion. IC50 values (listed in μM) were calculated using Graphpad Prism 6. The IC50 values of the drugs were determined in two biological experiments.