Histamine H1 assay (GDH14)

H1R functional mouse
Type of assay Cellular
Receptor: Mouse Histamine H1
Expression system: Transient transfection of HEK-293T
Reporter gene: NFAT-firefly luciferase
Radioligand concentration: 1.2 nM
Kd (nM): 1 nM
Experiment settings: - 8 concentrations of test compounds, each in triplicate
– total reaction volume of 200 µL
– 1 µM histamine (only for antagonism)
– incubation at 37°C for 6 hours
Read-out: Bioluminiscence
Reference: Histamine (EC50 = 186 nM)
Mepyramine (IC50 = 35 nM at 1 µM histamine)
Z’ factor >0.7