Affinity and functional potency of nelotanserin for human and rat 5-HT2 receptors
Values listed in this table comprise the mean ± S.E.M. of the indicated number of independent IC50 (radioligand-binding assay) and EC50 (IP accumulation assay) determinations (in parentheses). Triplicate determinations were performed at each of 8 to 10 different test compound concentrations. Ki values from radioligand competition studies were calculated from IC50 values.
| Receptor | [125I]DOI RBA Ki | IP Assay EC50 |
|---|---|---|
| nM | nM | |
| Human 5-HT2A | 0.4 ± 0.07 (29) | 0.9 ± 0.1 (13) |
| Human 5-HT2B | 2644 ± 147 (26) | 6856 ± 2575 (5) |
| Human 5HT2C | 106 ± 5 (27) | 30 ± 8 (4) |
| Rat 5-HT2A | 2.3 ± 1.0 (3) | 4.7 ± 0.4 (3)a |
| Rat 5-HT2B | 4,581 ± 278 (2) | ND |
| Rat 5-HT2C | 221 ± 23 (3) | 170 ± 39 (3)a |
RBA, radioligand-binding assay.
↵a Antagonist assay with 5 nM 5-HT (EC80) added before compound addition.