Identification and Characterization of ZEL-H16 as a Novel Agonist of the Histamine H3 Receptor
Figure 3
The selectivity of ZEL-H16 for hH3R in intracellular Ca2+ flux assay and CRE-luciferase transcription assay.
A–C, Intracellular Ca2+ flux or CRE-driven luciferase activity induced by ZEL-H16 in HEK-293 cells stably expressing hH1R (A), hH2R (B), or hH4R (C). D–F, The influence of ZEL-H16 on intracellular Ca2+ flux or CRE-driven luciferase activity induced by histamine in HEK-293 cells stably expressing hH1R(D), hH2R(E), or hH4R(F). The presented data points are the mean ±SE of triplicate values from a single experiment and are representative of three separate experiments. Statistical analysis between ZEL-H16 added or not added for each concentration point in the kinetic graph was done using a t-test (PRISM software). G, Relative expression of hH1R, hH2R, hH3R and hH4R on transfected HEK-293 cells by ELISA quantification for Flag-tagged cell-surface receptors (***p<0.001, compared to non-transfected HEK 293 cells).