Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

M1 receptor:9.5 nM(ki)

Clozapine减少独立于前脉冲抑制的大鼠阿朴吗啡治疗.Clozapine显示出'倒U'形的剂量-反应曲线,扭转阿朴吗啡引起的损耗前脉冲抑制.

Clozapine以浓度依赖性方式明显促进NMDA诱发的反应（EC50：14 nM）。Clozapine产生兴奋性突触后电位,被谷氨酸受体拮抗剂阻断,这表明这些兴奋性突触后电位是增加的兴奋性氨基酸的释放的结果。Clozapine是毒蕈碱M4受体的完全激动剂,EC50=11 nM,对forskolin刺激的cAMP累积产生抑制作用。Clozapine对其它4种毒蕈碱受体亚型的激动剂诱导的反应有强效拮抗作用。