Table 2.
Characterization of the binding of antihistamines to the H1R using competitive [3H]mepyramine binding experiments.
| pKi (37°C) | pKd,calc (25°C) | kon (25°C) (106⋅min-1⋅M-1) | koff (25°C) (min-1) | RTa (min) | |
|---|---|---|---|---|---|
| Mepyramine | 8.5 ± 0.0 | 8.8 ± 0.0 | 200 ± 50 | 0.28 ± 0.05 | 3.9 ± 0.6 |
| Levocetirizine | 8.1 ± 0.1 | 8.2 ± 0.1 | 1.2 ± 0.2 | 0.008 ± 0.001 | 140 ± 20 |
| Doxepin | 9.3 ± 0.1 | 9.1 ± 0.1 | 70 ± 10 | 0.06 ± 0.02 | 22 ± 7 |
| Olopatadine | 9.1 ± 0.0 | 8.5 ± 0.0 | 1.8 ± 0.1 | 0.006 ± 0.000 | 170 ± 10 |
| Triprolidine | 8.3 ± 0.1 | 8.1 ± 0.1 | 36 ± 5 | 0.30 ± 0.04 | 3.5 ± 0.4 |
| Acrivastine | 7.2 ± 0.0 | 7.0 ± 0.0 | 0.6 ± 0.1 | 0.065 ± 0.004 | 15.6 ± 0.9 |
| Desloratadine | 9.1 ± 0.1 | 9.5 ± 0.0 | 25 ± 12 | 0.008 ± 0.003 | 160 ± 50 |
| VUF14544 | 7.6 ± 0.1 | 7.8 ± 0.1 | 100 ± 40 | 1.3 ± 0.3 | 0.9 ± 0.2 |
| VUF14454 | 8.2 ± 0.1 | 8.6 ± 0.0 | 250 ± 90 | 0.6 ± 0.1 | 1.8 ± 0.3 |
| VUF14506 | 7.7 ± 0.1 | 7.9 ± 0.0 | 3.6 ± 0.7 | 0.05 ± 0.01 | 22 ± 4 |
| VUF14493 | 8.3 ± 0.0 | 8.4 ± 0.1 | 300 ± 100 | 0.9 ± 0.2 | 1.1 ± 0.2 |
Average values are shown ±SEM of ≥3 experiments.
aRT, residence time (1/koff).