| Assay Method Information | |
| | Determining 5-HT2A Binding Assay |
| Description: | Assays for determining 5-HT2A binding values were performed according to: Each of which is incorporated by reference in its entirety.Conc. Kd DetectionReceptors Source Ligand (nM) (nM) Non-specific Incubation Method5-HT2A (h) Human [3H] 0.5 0.6 Kentanserin 60 min rt Scintillation(antagonist recombinant kentanserin (1 μM) countingradioligand) (HEK-293 cells)Measured DetectionReceptors Source Stimulus Incubation component methodα1a (h) Human None rt Intracellular Fluorimetry(agonist recombinant (100 nM [Ca2+] effect) (CHO cells) epinephrine for control) α1a (h) Human Epinephrine rt Intracellular Fluorimetry(antagonist recombinant (3 nM) [Ca2+] effect) (CHO cells) α1b (h) Human None 30 min cAMP HTRF(agonist recombinant (100 nM 37° C. effect) (CHO cells) epinephrine for control) α1b (h) Human Epinephrine 30 min cAMP HTRF(antagonist recombinant (3000 nM) 37° C. effect) (CHO cells) α1d (h) Human None (1 μM rt Intracellular Fluorimetry(agonist recombinant epinephrine [Ca2+] effect) (CHO cells) for control) α1d (h) Human Epinephrine rt Intracellular Fluorimetry(antagonist recombinant (2.3 nM) [Ca2+] effect) (CHO cells)[0603]Results showing an inhibition (or stimulation for assays run in basal conditions) higher than 50% are considered to represent significant effects of the test compounds. 50% is the most common cut-off value for further investigation (determination of IC50 or EC50 values from concentration-response curves) that we would recommend. |
| Affinity data for this assay | |
|---|---|
| If you find an error in this entry please send us an E-mail | |