Curve fit parameters for antagonism of 5-HT (10 nM)-stimulated calcium signaling in HEK-293 cells expressing 5-HT2C-GFP Cells were preincubated for 30 min in the presence of the indicated inverse agonists and neutral antagonists and subsequently challenged with 10 nM 5-HT to assess antagonism. n is the number of independent experiments used to determine the mean ± S.E.M.
Function | Compound | IC50 ± S.E.M. | n |
|---|---|---|---|
| nM | |||
| Inverse agonist | SB-206553 | 106 ± 74 | 4 |
| Mianserin | 69 ± 42 | 4 | |
| Neutral antagonist | SB-242084 | 0.00015 ± 0.00005 | 3 |
|
| 5-Methoxygramine | 3150 ± 750 | 4 |