| Bioactivity | Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo[1][2]. |
| Invitro | Zotepine shows multiple antagonistic profiles with strong affinities to α1-adrenergic, α2-adrenergic, Dopamine D2, Histamine H1, Muscarinic, 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors, with Kds of 7.3, 180, 8, 3.3, 330, 280, 80, 2.6, 3.2 nM, respectively[1]. |
| In Vivo | Zotepine (1-3 mg/kg; a single i.p.) dose-dependently increases noradrenaline, dopamine, GABA, and glutamate release without affecting 5-HT levels in the medial prefrontal cortex of rats[2]. Animal Model: |
| Name | Zotepine |
| CAS | 26615-21-4 |
| Formula | C18H18ClNOS |
| Molar Mass | 331.86 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Richelson E, et, al. Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [2]. Yamamura S, et, al. Effects of zotepine on extracellular levels of monoamine, GABA and glutamate in rat prefrontal cortex. Br J Pharmacol. 2009 Jun;157(4):656-65. |