Zotepine

Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT_2A, 5-HT_2C, Histamine H₁, α₁-adrenergic and Dopamine D₂ receptors, with K_ds 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]. In Vitro: Zotepine shows multiple antagonistic profiles with strong affinities to α₁-adrenergic, α₂-adrenergic, Dopamine D₂, Histamine H₁, Muscarinic, 5-HT_1A, 5-HT_1D, 5-HT_2A, and 5-HT_2C receptors, with K_ds 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].