Cariprazine (hydrochloride)

Cariprazine is an atypical antipsychotic. 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 (sigma1) receptors (Kis = 0.085-23.44 nM). Cariprazine is an antagonist of dopamine D2 and D3 receptors (Kbs = 0.759 and 0.316 nM, respectively, in dopamine-induced [35S]GTPgammaS 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). 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.Formal Name: N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-dimethyl-urea, monohydrochloride. CAS Number: 1083076-69-0. Synonyms: RGH-188. Molecular Formula: C21H32Cl2N4O . HCl. Formula Weight: 463.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.5 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 217, 249 nm. SMILES: ClC1=C(Cl)C(N2CCN(CC[C@@H]3CC[C@@H](NC(N(C)C)=O)CC3)CC2)=CC=C1.Cl. InChi Code: InChI=1S/C21H32Cl2N4O.ClH/c1-25(2)21(28)24-17-8-6-16(7-9-17)10-11-26-12-14-27(15-13-26)19-5-3-4-18(22)20(19)23,/h3-5,16-17H,6-15H2,1-2H3,(H,24,28),1H/t16-,17-,. InChi Key: GPPJWWMREQHLQT-BHQIMSFRSA-N.