Histamine H4 assay (GDH48)

guinea pig H4R functional
Type of assay Biochemical
Receptor: Guinea pig histamine H4 receptor
Expression system: Transient transfection of HEK-293T
Radiotracer: 0.1 nM [35S]GTPγS
Experiment settings: - 8 concentrations of test compounds, each in triplicate
– total reaction volume of 100 µL
– 100 nM histamine (only for antagonism)
– incubation at RT for 1 hours
Read-out: Scintillation counting, converted in dpm unit
Reference agonist: Histamine (EC50 = 14 nM)
Thioperamide (IC50 = 1.4 µM at 0.1 µM histamine)
Z’ factor >0.5