Antagonistic activity of zotepine, norzotepine, and other antipsychotics in human H1 receptor functional assay
| Drugs | Corrected IC50 |
|---|---|
| nM | |
| Olanzapine | 1.1 ± 0.3 |
| Clozapine | 1.5 ± 0.6 |
| Chrolpromazine | 3.3 ± 1.9 |
| Zotepine | 8.0 ± 1.8 |
| Risperidone | 26 ± 0.9 |
| Norzotepine | 38 ± 11 |
| Haloperidol | >300 |
| Ziprasidone | >300 |
Stable H1 receptor-expressing cells were stimulated with histamine in the presence of compounds, and intracellular calcium release was measured in calcium flux assays using a fluorescent dye. Corrected IC50: IC50/(1 + [L]/EC50) (nM) with L as agonist concentration. Values are mean ± S.E.M. from three independent experiments.