TABLE 2

Antagonist effects in cellular functional assays (human receptors)

For assay details, see https://www.eurofinsdiscoveryservices.com/cms/cms-content/services/in-vitro-assays/.

AssaySourceMeasured ComponentStimulusIC50Kb
α2ACHO cellsBioimpedanceAdrenaline (100 nM)35 µM10 µM
α2CCHO cellsFluorescence (HTRF)Adrenaline (1 µM)n.c.an.c.a
5-HT7CHO cellscAMPSerotonin (300 nM)∼1000 µM
5-HT2AHEK-293 cellsIP1Serotonin (100 nM)150 µM21 µM
5-HT2CHEK-293 cellsIP1Serotonin (10 nM)3700 µM830 µM
  • a n.c.; IC50 not calculable. CHO, chinese hamster ovary; HEK, human embryonic kidney; HTRF, homogenous time-resolved fluorescence; IP, inositol phosphate.