TABLE 1
Affinity (pKi) of H4R ligands for different H4R species variants. The data are presented as mean ± S.E.M. of at least three independent experiments.
| Ligand | Structure | pKi at H4R species variant | ||||||
|---|---|---|---|---|---|---|---|---|
| Human | Monkey | Pig | Dog | Mouse | Rat | Guinea Pig | ||
| Histamine |  | 7.9 ± 0.1 | 7.8 ± 0.1 | 7.9 ± 0.1 | 7.2 ± 0.1 | 7.1 ± 0.1 | 7.0 ± 0.1 | 8.0 ± 0.1 |
| 4-MeHa |  | 7.3 ± 0.1 | 7.0 ± 0.1 | 7.7 ± 0.1 | 6.3 ± 0.1 | 6.8 ± 0.1 | 6.4 ± 0.1 | 7.3 ± 0.1 |
| VUF 8430 |  | 7.5 ± 0.1 | 7.3 ± 0.1 | 6.5 ± 0.1 | 5.9 ± 0.1 | 6.7 ± 0.1 | 6.8 ± 0.1 | 6.3 ± 0.1 |
| Clozapine |  | 6.4 ± 0.1 | 7.3 ± 0.1 | 5.2 ± 0.1 | 4.5 ± 0.1 | 5.5 ± 0.1 | 5.6 ± 0.2 | 7.3 ± 0.1 |
| Clobenpropit |  | 7.5 ± 0.1 | 7.5 ± 0.1 | 6.6 ± 0.1 | 6.5 ± 0.1 | 7.3 ± 0.1 | 7.3 ± 0.1 | 8.2 ± 0.1 |
| JNJ 7777120 |  | 8.3 ± 0.1 | 7.5 ± 0.1 | 6.3 ± 0.1 | 7.1 ± 0.1 | 8.4 ± 0.1 | 8.4 ± 0.1 | 6.0 ± 0.1 |
| VUF 6002 |  | 7.5 ± 0.1 | 6.7 ± 0.1 | 5.1 ± 0.1 | 6.2 ± 0.1 | 6.9 ± 0.1 | 7.3 ± 0.1 | 5.8 ± 0.1 |
| Thioperamide |  | 7.1 ± 0.1 | 7.1 ± 0.1 | 7.0 ± 0.1 | 6.4 ± 0.1 | 7.6 ± 0.1 | 7.5 ± 0.1 | 7.1 ± 0.1 |