Active cyamemazine metabolites in patients treated with cyamemazine (Tercian®): influence on cerebral dopamine D2 and serotonin 5-HT2A receptor occupancy as measured by positron emission tomography (PET)

摘要

Cyamemazine (Tercian®) is an antipsychotic agent blocking central dopamine D2 receptors, which induces few extrapyramidal adverse effects, due to a potent antagonistic action at serotonin 5-HT2A receptors. In vitro studies showed that the desmethyl metabolite of cyamemazine (N-desmethyl cyamemazine) has similar affinity for 5-HT2A receptors as cyamemazine, whereas its D2 receptor affinity is eight times lower (Benyamina et al. in Eur J Pharmacol 578(2–3):142–147, 2008). Moreover, cyamemazine sulfoxide showed modest affinity for 5-HT2A receptors.