Clozapine (HF 1854) dihydrochloride is utilized for researching psychiatric disorders. This compound exhibits high affinity for numerous neuroreceptors and acts as an effective antagonist of dopamine receptors, with a Ki value of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor, with Ki values of 9.5 nM and 4 nM, respectively. Additionally, Clozapine is a selective agonist of the muscarinic M4 receptor (EC50 = 11 nM).

α2-adrenergic receptor:51 nM (Ki), 5-HT2A receptor:4 nM (Ki), D2 Receptor:75 nM (Ki), mAChR4:11 nM (EC50), mAChR1:9.5 nM (Ki)

Clozapine (HF 1854) 是一种 D2 受体拮抗剂，其 K i 为 75 nM，并作用于血清素 5HT2A 受体，K i 为 4 nM，同时抑制毒蕈碱 M1 受体，K i 为 9.5 nM，并阻断 α2-肾上腺素受体，K i 为 51 nM。在 HeLa 细胞中，Clozapine (0-1 μM；24 h) 下调 5-HT 6 并上调 5-HT 7 受体。此外，Clozapine 对在 CHO 细胞中表达的毒蕈碱 M4 受体表现为完全激动剂，其 EC 50 为 11 nM。

氯氮平 (HF 1854)（25 mg/kg/天；腹腔注射；21 天）在麦角酸二乙胺诱导的精神病小鼠模型中体现出显著的抗精神病效应。