In vitro and in vivo potencies of H3-receptor antagonists
| Compounds | In Vitro Tests (Ki , nM) | In Vivo Test (ED50, mg/kg, p.o.) | ||
|---|---|---|---|---|
| [3H]HA release1-a | [125I]Iodoproxyfan binding1-b | Increase in t-MeHA level in mouse brain1-c | ||
| Ciproxifan | 0.5 ± 0.1 | 0.7 ± 0.2 | 0.14 ± 0.03 | |
| Thioperamide | 4 ± 1 | 4 ± 1 | 1.0 ± 0.5 | |
| Carboperamide | 20 ± 2 | 6 ± 2 | 3.9 ± 0.8 | |
| Clobenpropit | 0.6 ± 0.2 | 0.5 ± 0.1 | ∼25 | |
| Iodoproxyfan | 5 ± 1 | 0.2 ± 0.1 | >25 | |
↵1-a Data from Fig. 3 except for thioperamide (from Arranget al., 1987) and iodoproxyfan (from Ligneau et al., 1994).
↵1-b Data from Ligneau et al. (1994) except for ciproxifan (fig. 4).
↵1-c Data from figure 8 except for thioperamide (from Ganellinet al., 1996) and iodoproxyfan (from Stark et al., 1996).