| Assay Method Information | |
| | 5HT1A Competitive Binding Assay |
| Description: | Competitive binding assay (Eurofins Cerep) was performed using human recombinant 5-HT1A transfected to HEK-293 cells, [3H]8-OHDPAT (0.5 nM) and the test compound from Example 1 was tested at 8 concentrations ranging from 0.01 mM to 30 mM (Choi D S et al. FEBS Letters 1994, 352, 393). The analysis was performed using software developed at Cerep (Hill software) and validated by comparison with data generated by the commercial software SigmaPlot 4.0 for Windows ( 1997 by SPSS Inc). The binding constant (Ki 540 nM) were calculated using the Cheng Prusoff equation. The compound is a modest agonist at the 5HT1A receptor, but prefers the 5HT2A receptor (Ki 110 nM) by about 5-fold selectivity. |
| Affinity data for this assay | |
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