Table 3.
Emax and pEC50 values of several 5-HT6 receptor ligands for inducing cAMP formation in transiently transfected COS-7 cells with either human wild-type or S267K mutant 5-HT6 receptor
| cAMP formation | ||||
|---|---|---|---|---|
| 5-HT6 receptor | Wild-type | S267K | ||
| Compound | Emax (pmol 106 cells−1) | pEC50 | Emax (pmol 106 cells−1) | pEC50 |
| 5-HT | 18.3±0.6 | 8.31±0.16 | 19.1±0.3 | 8.73±0.25 |
| E-6801 | 19.6±0.6 | 9.50±0.21 | 18.5±0.3 | 9.40±0.14 |
| E-6837 | 17.6±0.5 | 9.89±0.21 | 19.4±0.4 | 9.31±0.18 |
| SB-271046 | 6.3±0.2 | <5 | 5.9±0.4a | 8.69±0.36 |
| Ro 04-6790 | 6.7±0.3 | <5 | 6.5±0.7b | 7.13±0.78 |
| Basal | 6.8±0.2 | — | 9.7±0.4c | — |
Emax and pEC50 values were derived from cAMP-mediated agonist/inverse agonist curves as illustrated in Figure 7. Data correspond to mean±s.e.m. values of five to ten independent experiments performed in duplicate. a: P<0.001 versus basal value of mutant 5-HT6 receptor; b P<0.01 versus basal value of mutant 5-HT6 receptor; c: P<0.001 versus basal value of wild-type 5-HT6 receptor.