Receptor affinities.
Panel screens of up to 105 radioligand-binding assays and 34 enzyme assays were performed, and the affinity of SEP-856 was determined for receptors at which >50% inhibition was seen at 10 μM. Details of radioligands, incubation conditions , and the targets in the screening panels are listed in the Supplemental Material. Data are shown as mean ± S.E.M. (n ≥ 3, n = 1 for 5-HT2B).
Receptor | Ki (µM) |
---|---|
D2s | 21.3 ± 8.2 |
5-HT1A | 0.284 ± 0.056 |
5-HT1B | 1.90 ± 1.72 |
5-HT1D | 1.13 ± 0.21 |
5-HT2A | 17.25 ± 4.0 |
5-HT2B | 1.1 |
5-HT2C | 2.45 ± 0.82 |
5-HT7 | 0.031 ± 0.003 |
α2A | 0.59 ± 0.06 |
α2B | 1.9 ± 0.10 |