Table 1.
Binding affinities of the selected compounds towards serotonin receptors.
| Receptor | Compound 2a Ki (nM) | Compound 2c Ki (nM) | Compound 2d Ki (nM) | Compound 2e Ki (nM) | Controls | |
|---|---|---|---|---|---|---|
| Ergotamine Ki (nM) | Methysergide Ki (nM) | |||||
| 5-HT1A | 110.0 ± 17.0 | 5.5 ± 0.4 | 9.6 ± 1.1 | 130.0 ± 16.0 | 0.17 | 14.0 |
| 5-HT1B | 66.0 ± 9.0 | 66.0 ± 5.0 | 19.0 ± 2.0 | 43.0 ± 5.0 | 0.3 | 2.5 |
| 5-HT1D | 29.3 ± 3.7 | 14.0 ± 1.0 | 2.6 ± 0.32 | 8.5 ± 1.38 | 0.3 | 69.0 |
| 5-HT1E | >10,000 | 356.0 ± 34.0 | 398.0 ± 30.0 | 310.0 ± 33.0 | 19.0 | 237.0 |
| 5-HT2B | 145.0 ± 13.0 | 7.8 ± 0.7 | 27.0 ± 1.0 | 98.0 ± 4.0 | 1.9 | 0.1 |
| 5-HT3 | 5,187 ± 883 | 1,325 ± 125 | 1,374 ± 212 | 4,486 ± 804 | >10,000 | >10,000 |
| 5-HT5A | >10,000 | 408.0 ± 54.0 | 1,038 ± 110 | 1,254 ± 197 | - | >10,000 |
| 5-HT6 | 189.5 ± 32.5 | 30.0 ± 2.0.0 | 22.0 ± 2.0 | 198.0 ± 20.0 | 12.0 | 52.0 |
| 5-HT7 | 77.0 ± 16.0 | 7.2 ± 0.6 | 8.3 ± 0.9 | 116.0 ± 13.0 | 1,291 | 30.0 |