TABLE 2
Antagonist effects in cellular functional assay (human receptors)
For assay details, see https://www.eurofinsdiscoveryservices.com/cms/cms-content/services/in-vitro-assays/.
| Assay | Source | Measured Component | Stimulus |  |  |
|---|---|---|---|---|---|
| α2A | CHO cells | Bioimpedance | Adrenaline(100 nM) | 35 μM | 10 μM |
| α2C | CHO cells | Fluorescence(HTRF) | Adrenaline(1 μM) | n.c.a | n.c.a |
| 5-HT7 | CHO cells | cAMP | Serotonin(300 nM) | ∼1000 μM | |
| 5-HT2A | HEK-293 cells | IP1 | Serotonin(100 nM) | 150 μM | 21 μM |
| 5-HT2C | HEK-293 cells | IP1 | Serotonin(10 nM) | 3700 μM | 830 μM |
↵a n.c.;
not calculable. CHO, chinese hamster ovary; HEK, human embryonic kidney; HTRF, homogenous time-resolved fluorescence; IP, inositol phosphate.