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Zotepine is an atypical antipsychotic.1 It is a dopamine D2 and D3 receptor antagonist (Kis = 5.37 and 6.45 nm, respectively) that reverses dopamine inhibition of forskolin-stimulated cAMP production in CHO cells expressing human D2 and D3 receptors. In vivo, zotepine inhibits head twitches induced by 5-hydroxy-L-tryptophan (Item No. 20539), a behavior mediated by the serotonin (5-HT) receptor subtype 5-HT2, in mice (ED50 = 0.13 mg/kg).2 It acts as an α2-adrenergic receptor (α2-AR) antagonist, reducing the hind limb flexor reflex stimulated by clonidine (Item No. 15949) in rats. Zotepine blocks gnawing behavior and body turning induced by apomorphine (Item No. 16094) and methamphetamine in rats.3 It also induces catalepsy and inhibits apomorphine-induced vomiting in dogs. Formulations containing zotepine have been used in the treatment of schizophrenia and acute mania.
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1. Effects of recent and reference antipsychotic agents at human dopamine D2 and D3 receptor signaling in Chinese hamster ovary cells. Psychopharmacology (Berl.) 150(4), 383-390 (2000).
2. Pharmacological effects of zotepine and other antipsychotics on the central 5-
3. Effects of microinjection of 2-