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Desmethyl cariprazine (DCAR) is the primary active metabolite of the atypical antipsychotic drug cariprazine. It is formed in the liver primarily by the cytochrome P450 enzyme CYP3A4 and to a lesser extent by CYP2D6. DCAR, along with didesmethyl cariprazine, significantly contributes to the overall clinical efficacy of cariprazine. It acts as a partial agonist at dopamine D3 and D2 receptors, with a notable preference for D3 receptors, and also as a partial agonist at serotonin 5-HT1A receptors. Additionally, it functions as an antagonist at serotonin 5-HT2B and 5-HT2A receptors. This pharmacological profile allows it to modulate dopaminergic and serotonergic neurotransmission, contributing to the therapeutic effects observed in conditions such as schizophrenia and bipolar disorder.
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