TABLE 3
Pharmacological analysis of chimeric human and mouse H4R proteins 7 to 10, using [3H]histamine saturation analysis and displacement studies Equilibrium Kd and Bmax values for [3H]histamine (picomole per milligram protein) and pKi of all ligands tested at chimeras 7 to 10 are presented as average ± S.E.M. of results of at least three independent experiments.
Receptor | Kd | Bmax | pKi | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Histamine | Clozapine | VUF 8430 | |||||||
| nM | |||||||||
| hH4R |
| 9.0 ± 0.1 | 2.71 ± 1.00 | 7.89 ± 0.05 | 6.35 ± 0.03 | 7.46 ± 0.02 | |||
| mH4R |
| 77.5 ± 11 | 1.48 ± 0.24 | 7.09 ± 0.04 | 5.49 ± 0.07 | 6.75 ± 0.10 | |||
| Chimera 7 |
| 7.4 ± 0.7 | 1.57 ± 0.42 | 7.96 ± 0.08 | 6.57 ± 0.06 | 7.56 ± 0.12 | |||
| Chimera 8 |
| 91.2 ± 9.1 | 1.20 ± 0.28 | 7.22 ± 0.08 | 5.56 ± 0.12 | 6.64 ± 0.06 | |||
| Chimera 9 |
| 9.2 ± 2.3 | 3.28 ± 0.53 | 7.75 ± 0.04 | 6.22 ± 0.04 | 7.48 ± 0.11 | |||
| Chimera 10 |
| 79.4 ± 6.5 | 1.60 ± 0.58 | 6.93 ± 0.19 | 5.40 ± 0.04 | 7.05 ± 0.08 | |||