Assay Method Information

Assay Name:  Determination of Ki Value at 5-HT2A Receptor
Description:  Compound was tested according to the following procedures.Materials and Methods:Receptor source: Recombinant mammalian cellsRadioligand: [3H]-Ketanserine (47.3 Ci/mmol)Final ligand concentration [1.75 nM]Non-Specific Ligand: 0.1 mM 1-Naphthylpiperazine (1-NP)Reference compound: 1-Naphthylpiperazine (1-NP)Positive control: 1-Naphthylpiperazine (1-NP)Incubation conditions: Reactions were carried out in 67 mM Tris-HCl (pH 7.4) for 1 hour 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-HT2A binding site.Reference: Methods in Molecular Biology, 2002, 190, 31-49Compounds 1, 2 and 3 bind weakly to 5-HT2A receptor when tested by the in-vitro radioligand binding technique on human recombinant 5-HT2A receptor.
Affinity data for this assay
 

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