Cariprazine

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.

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1. Mészáros, G.P., Agai-Csongor, E., and Kapás, M. Sensitive LC-MS/MS methods for the quantification of RGH-188 and its active metabolites, desmethyl- and didesmethyl-RGH-188 in human plasma and urine. J. Pharm. Biomed. Anal. 48(2), 388-397 (2008).

2. Kiss, B., Horváth, A., Némethy, Z., et al. Cariprazine (RGH-188), a dopamine D₃ receptor-preferring, D₃/D₂ dopamine receptor antagonist-partial agonist antipsychotic candidate: In vitro and neurochemical profile. J. Pharmacol. Exp. Ther. 333(1), 328-340 (2010).

3. Gyertyán, I., Kiss, B., Sághy, K., et al. Cariprazine (RGH-188), a potent D₃/D₂ dopamine receptor partial agonist, binds to dopamine D₃ receptors in vivo and shows antipsychotic-like and procognitive effects in rodents. Neurochem. Int. 59(6), 925-935 (2011).