| Assay Method Information | |
| | Human Serotonin Transporter (SERT, SLC6A4) Functional Antagonist Uptake Assay |
| Description: | Benzofuran derivatives were evaluated for inhibiting the human 5-HT transporter (hSERT) as expressed in CHO cells using an antagonist radioligand assay (Tatsumi, M. et al. (1999), Eur. J. Pharmacol., 368: 277-283). Compound binding was calculated as a percent inhibition of the binding of 2 nM [3H]imipramine using a scintillation method and inhibition constants (Ki) were calculated using the Cheng Prusoff equation. Test compounds were assayed in three trials at 300, 94.868, 30, 9.4868, 0.3, and 0.94868 μM.[2927]All tested compounds showed inhibition of hSERT at the tested concentrations. However, in two cases (the enantiomers of 5-MBPB), the lowest concentration of 0.94868 μM was too high to accurately estimate IC50 values and Ki values. For S-(+)-5-MBPB the IC50 appeared close to 0.094868 μM, while for R-(−)-5-MBPB the IC50 appeared close to 0.94868 μM. |
| Affinity data for this assay | |
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