Formulation: A solid
Formal Name: N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-di(methyl-d3)-urea
Purity: ≥99% deuterated forms (d1-d6)
Formula Markup: C21H26D6Cl2N4O
Formula Weight: 433,5
Shelf life (days): 1460
CAS Number: 1308278-67-2
Notes: Cariprazine-d6 is intended for use as an internal standard for the quantification of cariprazine (Item Nos. 31446 / 24025) by GC- or LC-MS. Cariprazine is an atypical antipsychotic.{60050} It binds to dopamine D2L, D2S, and D3 receptors, the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2B, and histamine H1 and sigma-1 (σ1) receptors (Kis = 0.085-23.44 nM).{36514} Cariprazine is an antagonist of dopamine D2 and D3 receptors (Kbs = 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 D2L 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).{60051} 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.
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