Table 1. Selective antagonists of TPH1, SERT and 5-HT receptors inhibit tumorsphere formation by HCC1954 breast tumor cells.
| Target | Compound | IC50 |
|---|---|---|
| TPH1 | LP-533401 | 6.1 |
| SERT | Paroxetine | 2.7 |
| Fluoxetine | 3.4 | |
| Sertraline | 1.1 | |
| 5-HT1B | SB-224289 | 0.4 |
| 5-HT1D | GR-127935 | 4.8 |
| 5-HT2A | 4F-4PP | 2.2 |
| 5-HT2B | RS-127445 | 10.6 |
| SB-204741 | 8.2 | |
| 5-HT2C | SB-242084 | 0.6 |
| 5-HT4 | GR-113808 | 16.9 |
| SB-204070 | 22.3 | |
| 5-HT5A | SB-699551 | 0.3 |
| 5-HT6 | NPS ALX 4a | 1.0 |
| SB-258585 | 9.1 | |
| 5-HT7 | SB-258719 | 14.0 |
Human HCC1954 cells were grown in the presence of serial dilutions of each selective antagonist. Over a four-day incubation many of the antagonists reduced sphere formation in a dose-dependent fashion. IC50 values (listed in μM) were calculated using Graphpad Prism 6. The activity of selective antagonists were determined in two biological experiments.