Histamine H3 assay (GDH32)

human H3R functional
Type of assay Biochemical
Receptor: Human histamine H3
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
– 1 µM histamine (only for antagonism)
– incubation at RT for 1 hours
Read-out: Scintillation counting, converted in dpm unit
Reference agonist: Histamine (EC50 = 54 nM)
Thioperamide (IC50 = 292 nM at 1 µM histamine)
Z’ factor >0.5