Zuclopenthixol antagonises both dopamine D and D receptors, α-adrenoceptors and 5-HT receptors with a high affinity, but has no affinity for muscarinic acetylcholine receptors. It weakly antagonises the histamine (H) receptor but has no α-adrenoceptor blocking activity .
Evidence from in vitro work and clinical sources (i.e. therapeutic drug monitoring databases) suggests that both CYP2D6 and CYP3A4 play important roles in zuclopenthixol metabolism.