Table 3.
EC/IC50 and E/IMAX values of ligands to activate/inactivate 5-HT2C receptor-mediated phospholipase C signaling. Functional assays were performed in HEK cells transiently expressing WT, S3.36A or Y7.43A 5-HT2C receptors. EMAX/IMAX values represent percent change from baseline. Data shown are means and S.E.M. (shown in parentheses) of at least 3 independent experiments performed with triplicates. EC/IC50 fold change represents the quantitative fold difference between EC/IC50 values of WT and S3.36A or WT and Y7.43A 5-HT2C receptors, respectively.
| LIGAND | WT 5-HT2C | S3.36A | Y7.43A | FOLD CHANGE |
|||
|---|---|---|---|---|---|---|---|
| EC/IC50 (nM) |
E/Imax | EC/IC50 (nM) |
E/Imax | EC/IC50 (nM) |
E/Imax | EC/IC50 | |
| Serotonin | 5.5 (1.3) | 204.7 (11.6) | 289.1 (40.4)a |
998.4 (137.1)b |
158.7 (19.9)a |
223.4 (22.7) | 52.6, 28.9 |
|
N(CH3)2- PAT |
61.1 (18.2) | 163.0 (9.7) | 682.5 (102.5)a |
588.0 (62.0) b |
519.7 (98.8)a |
180.8 (14.2) |
11.2, 8.5 |
| Mesulergine | 23.9 (8.3) | 82.9 (1.9) | 19.9 (8.2) | 152.0 (9.2)b | 38.9 (13.3) | 79.3 (2.5) | 0.8, 1.6 |
significantly different from WT 5-HT2C.