Table 1

Ligand affinities for the H4 receptor

−LogEC50(Ki)Hill Coefficient
nM
Amitriptyline7.31  ± 0.26 (33.6)0.8
Chlorpromazine7.13  ± 0.29 (50.2)0.7
Doxepin6.79  ± 0.13 (105.9)0.6
Cinnarizine6.73  ± 0.20 (141.6)0.7
Promethazine6.71  ± 0.19 (150.2)0.6
Cyproheptadine6.53  ± 0.09 (201.5)0.9
Clemizole6.16  ± 0.12 (402.2)0.5
Mianserin5.96  ± 0.40 (750.0)0.9
Clozapine5.90  ± 0.22 (849.6)1.2
Chlorpheniramine5.39  ± 0.16 (2910.0)1.1
Histamine5.30  ± 0.04 (3442.3)0.5
Imetit5.25  ± 0.44 (3795.6)0.2
Pheniramine5.21  ± 0.47 (4184.0)0.2
Dimaprit4.76  ± 0.19 (11812.7)0.4
α-Methylhistamine>10,000Undetermined
Cimetidine>10,000Undetermined

Data represent mean ± S.E. for two to four separate experiments. Twelve different concentrations spanning 6 log units of test drug were used to displace 15 nM [3H]pyrilamine.