| Assay Method Information | |
| | 5-HT2A and 5-HT2B Receptor Binding |
| Description: | The binding affinities of disclosed compounds at the ketanserin binding site of the 5-HT2A receptor and the LSD binding site of the 5-HT2B receptor were determined in radioligand binding experiments.Methods:[0631]Affinity of the test compounds for the 5-HT2A receptor was determined in radioligand binding experiments with [3H]ketanserin by WuXi AppTec (Hong Kong) Limited, using methods adapted from the literature and under conditions described in Table 1.TABLE 1Assay conditions for 5-HT2A receptor radioligand binding.Receptor Source HEK293 stable cell lineIncubation Vehicle 0.5% DMSOIncubation Time 1 hIncubation Temperature25° C.Incubation Buffer50 mM Tris-HCl, pH 7.4Ligand 1 nM [3H]ketanserinNon-Specific Ligand 1 μM ketanserin[0632]Affinity of the test compounds for the 5-HT2B receptor was determined in radioligand binding experiments with [3H]LSD by WuXi AppTec (Hong Kong) Limited, using methods adapted from the literature and under conditions described in Table 2.TABLE 2:Assay conditions for 5-HT2B receptor radioligand binding.Receptor Source HEK293 stable cell lineVehicle 1.0% DMSOIncubation Time 1 hIncubation Temperature25° C.Incubation Buffer50 mM Tris-HCl, pH 7.4Ligand 1 nM [3H]LSDNon-Specific Ligand50 μM serotoninResults:Results of the radioligand binding assays are shown in Table 3. Tested compounds showed substantial binding affinity for the 5-HT2A and 5-HT2B receptor. Compounds having the R configuration at position 9 were much more potent at the 5-HT2A receptor than those having the S configuration at this position. Tested compounds were more selective for the 5-HT2A receptor over the 5-HT2B receptor compared to the reference compound LSD. |
| Affinity data for this assay | |
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