Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine ( HY-14763 ). Didesmethyl cariprazine is a partial agonist at the D 2 and D 3 receptors, full agonist at the 5-HT 1A receptor, and antagonist at the human 5-HT 2B receptor ( K i : 1.41 nM (human D 2L ), 0.056 nM (human D 3 ), 1.7 nM (human 5-HT 1A ), 0.52 nM (human 5-HT 2B )). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
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