Table 3.
Binding affinities of 5-HT4 ligands 8, 13 and 17 for non-serotonergicreceptors and binding sites.
| Binding site or receptor | Binding affinities (Ki) (nM) |
||
|---|---|---|---|
| Ligand 8 | Ligand 13 | Ligand 17 | |
| hα1A | 522 | >10,000 | 87.6 |
| hα1B | >10,000 | 4,228 | 9,076 |
| hα1D | 2,276 | >10,000 | >10,000 |
| hα2A | 2,239 | >10,000 | >10,000 |
| hα2B | 671.2 | >10,000 | 773 |
| hα2C | 556 | 989 | 593 |
| β1 (rat) | >10,000 | 4,407 | >10,000 |
| β2 (rat) | >10,000 | >10,000 | >10,000 |
| β3 (rat) | >10,000 | >10,000 | >10,000 |
| σ1 (rat) | 60 | 211 | 55 |
| σ2 (rat) | 8 | 148 | 12.9 |
| BZP (rat brain site) | >10,000 | >10,000 | >10,000 |
| hDAT | 2,020 | >10,000 | >10,000 |
| hDOR | >10,000 | >10,000 | >10,000 |
| D1 (rat) | 2,291 | >10,000 | >10,000 |
| D2 (rat) | 220 | >10,000 | 615 |
| D3 (rat) | 336 | 6,272 | 1,011 |
| D4 (rat) | 43 | 1,272 | 316 |
| hD5 | 972 | >10,000 | >10,000 |
| hGABAA | >10,000 | >10,000 | >10,000 |
| H1 (guinea pig) | 2,727 | >10,000 | >10,000 |
| H2 (guinea pig) | >10,000 | >10,000 | >10,000 |
| H3 (guinea pig) | >10,000 | 1,649 | 5,038 |
| H4 (guinea pig) | >10,000 | >10,000 | >10,000 |
| hKOR | >10,000 | >10,000 | >10,000 |
| hMOR | >10,000 | >10,000 | >10,000 |
| hM1 | >10,000 | >10,000 | >10,000 |
| hM2 | 433 | >10,000 | >10,000 |
| hM3 | 823 | 1,095 | >10,000 |
| hM4 | 760 | 2,579 | >10,000 |
| hM5 | 972 | 4,058 | >10,000 |
| hNET | 3,226 | >10,000 | >10,000 |