In vitro functional profile of SEP-856.
The functional effects of SEP-856 were determined for receptors at which >50% inhibition was seen in the panel screens. The in vitro pharmacology studies were run in both agonist and antagonist modes. The specific assays are listed in Materials and Methods. Data are shown as mean ± S.E.M. (n ≥ 3).
| Receptor | Agonist | Antagonist | ||
|---|---|---|---|---|
| EC50 (µM) | % Emax | IC50 (µM) | % Inhibition | |
| TAAR1 | 0.140 ± 0.062 | 101.3 ± 1.3 | NE | NE |
| 5-HT1A | 2.3 ± 1.40 | 74.7 ± 19.6 | NE | NE |
| 5-HT1B | 15.6 ± 11.60 | 22.4 ± 10.9 | NE | NE |
| 5-HT1D | 0.262 ± 0.09 | 57.1 ± 6.0 | NE | NE |
| 5-HT2A | >10 | 29.3 @ 10 μM | NE | NE |
| 5-HT2C | 30 ± 4.5 | 63.3 ± 3.1 | NE | NE |
| 5-HT7 | 6.7 ± 1.32 | 41.0 ± 9.5 | NE | NE |
| α2A | >10 | 39.4 ± 4.2 | NE | NE |
| α2B | NE | NE | NE | NE |
| D2L (cAMP) | 10.44 ± 4.0 | 23.9 @ 10 μM | >100 | 34.0 ± 1.16 |
| D2L (arrestin recruitment) | 8.02 | 27.1 @ 10 μM | >100 | <25 @ 100 µM |
NE, no effect (<30% @ 30 µM).