| Assay Method Information | |
| | Determination of Ki Value at 5-HT6 Receptor |
| Description: | Compound was tested at MDS pharma services and Novascreen according to the following procedures.Materials and Methods:Receptor source: Human recombinant expressed in Hela cellsRadioligand: [3H]-LSD (60-80 Ci/mmol)Final ligand concentration [1.5 nM]Non-Specific Ligand: 5 μM Serotonin (5-HT)Reference compound: Methiothepin mesylatePositive control: Methiothepin mesylateIncubation conditions: Reactions were carried out in 50 mM Tris-HCl (pH 7.4) containing 10 mM MgCl2, 0.5 mM EDTA for 60 minutes at 37° C. The reaction was terminated by rapid vacuum filtration onto the glass fiber filters. Radioactivity trapped onto the filters was determined and compared to the control values in order to ascertain any interactions of the test compound(s) with the cloned serotonin 5-HT6 binding site.Reference: Molecular Pharmacology, 1993, 43, 320-327.Compounds 1, 2 and 3 selectively bind to 5-HT6 receptor when tested by the in-vitro radioligand binding technique on human recombinant 5-HT6 receptor. |
| Affinity data for this assay | |
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