Didesmethyl cariprazine

Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D₂ and D₃ 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 D₃), 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^[1][2]. In Vitro:Didesmethyl cariprazine is a partial agonist of D₂ and D₃ receptors, a full agonist of the 5-HT_1A receptor, and an antagonist of the human 5-HT_2B receptor (K_i: 1.41 nM (human D_2L)), 0.056 nM (human D₃), 1.7 nM (human 5-HT_1A), 0.52 nM (human 5-HT_2B))^[2]. In Vivo:Didesmethyl cariprazine (120 μg/kg; i.v.) dose-dependently but partially suppresses the spontaneous activity of midbrain dopaminergic neurons in rats^[2].