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Pharmacological profiles of compound (+)-1 and (±)-2.a
| Compound | EC50, nM (Emax; % 5-HT) | ||
|---|---|---|---|
| 5-HT2C | 5-HT2B | 5-HT2A | |
| 5-HT | 0.20 (100%) | 1.3 (100%) | 2.1 (100%) |
| (+)-1 (TFA salt) | 71 (100%) | 682 (57%) | 7190 (17%) |
| (±)-2 (HCl salt) | 600 (66%) | NA | NA |
Functional data was acquired with recombinantly expressed human serotonin receptors in HEK-293 (5-HT2A and 5-HT2B) and PO1C (5-HT2C) cell lines, fluorescence imaging plate reader (FLIPR) assay; “NA”, no activity at 10 µM.
