In vitro binding profiles of ligands for 5-HT2AR, 5-HT2BR, and 5-HT2CR
| Ligand | 5-HT2 Receptor Family | ||
|---|---|---|---|
| Affinity Ki | |||
| Antagonistsa | h5-HT2AR | h5-HT2BR | h5-HT2CR |
| nM | |||
| Ketanserin | 8.1 | 741 | 62 |
| M100907 | 1.9 | 1000 | 30 |
| Pimavanserin | 0.05 | N.D. | 1.6 |
| SB 242084 | 851 | 145 | 7.1 |
| SB 243213 | 160 | 100 | 1.0 |
N.D., not determined.
↵a Published studies employed radioligand binding assays to establish the affinity (Ki) of ketanserin, M100907 (MDL100907), SB 242084, and SB 243213 for the 5-HT2R subtypes in h5-HT2AR–, h5-HT2BR–, or h5-HT2CR–transfected HEK-293 and h5-HT2BR–transfected CHO-K1 clonal cell lines (Bromidge et al., 2000; Knight et al., 2004). Pimavanserin binding affinity for the 5-HT2R subtypes was determined in NIH-3T3 cells (Vanover et al., 2006).