Cariprazine-d6

Properties

Safety Information

Description

Cariprazine-d₆ is intended for use as an internal standard for the quantification of cariprazine by GC- or LC-MS. Cariprazine is an atypical antipsychotic.¹ It binds to dopamine D_2L, D_2S, and D₃ receptors, the serotonin (5-HT) receptor subtypes 5-HT_1A, 5-HT_2A, and 5-HT_2B, and histamine H₁ and sigma-1 (σ₁) receptors (K_is = 0.085-23.44 nM).² Cariprazine is an antagonist of dopamine D₂ and D₃ receptors (K_bs = 0.759 and 0.316 nM, respectively, in dopamine-induced [³⁵S]GTPγS binding assays). It is also a partial agonist at these receptors, stimulating inositol phosphate production in murine A9 cells expressing human D_2L receptors (EC₅₀ = 3.16 nM) and inhibiting forskolin-induced cAMP accumulation in CHO cells expressing human D₃ receptors (EC₅₀ = 2.63 nM). Cariprazine inhibits amphetamine-induced hyperactivity and the conditioned avoidance response in rats (ED₅₀s = 0.12 and 0.84 mg/kg, respectively).³ It also inhibits scopolamine-induced learning deficits in a water labyrinth learning test in rats when administered at doses ranging from 0.02 to 0.08 mg/kg. Formulations containing cariprazine have been used in the treatment of schizophrenia, as well as manic, depressive, or mixed episodes associated with bipolar I disorder.