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 is a second-generation antipsychotic with a primary use as a treatment for schizophrenia, although clinical trials have been conducted into its efficacy as an antimanic agent in patients with acute bipolar mania.

H1 receptor:3.3 nM(Kd), 5-HT2A:2.6 nM(Kd), 5-HT2C:3.2 nM(Kd)