Table 2.
The results from functional assays towards 5-HT6R and 5-HT2AR for compounds 1–3.
| Target | 5-HT2AR | 5-HT6R | ||
|---|---|---|---|---|
| Compound | Agonist Mode * Emax [%] ± SEM | Antagonist Mode ** pKb ± SEM | Agonist Mode * Emax [%] ± SEM | Antagonist Mode *** pKb ± SEM |
| Serotonin | 100.00 ± 0.30 | N.C. | 100.00 ± 0.5 | N.C. |
| Mianserin | 1.00 ± 0.30 | 9.70 ± 0.12 | 2.00 ± 0.50 | 6.08 ± 0.05 |
| SB258585 | N.T. | N.T. | 2.00 ± 0.50 | 8.92 ± 0.10 |
| 1 | 58.00 ± 9.70 | N.C. | 4.00 ± 0.00 | 10.57 ± 0.07 |
| 2 | 21.00 ± 0.60 | 8.61 ± 0.03 | 5.00 ± 1.10 | 8.19 ± 0.33 |
| 3 | N.T. | N.T. | 9.00 ± 1.40 | 7.67 ± 0.20 |
* Results were normalized as percentage of maximal agonist response (Serotonin 10−5 M). ** Results were normalized as percentage of maximal response in the absence of antagonist. *** Results were normalized as percentage of reference antagonist (SB258585 10−5 M). Emax is the maximum possible effect. N.C.—not calculable. N.T.—not tested.