Description
Cariprazine-d
6 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 D
3 receptors, the serotonin (5-HT) receptor subtypes 5-HT
1A, 5-HT
2A, and 5-HT
2B, and histamine H
1 and sigma-1 (σ
1) receptors (K
is = 0.085-23.44 nM).
2 Cariprazine is an antagonist of dopamine D
2 and D
3 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 (EC
50 = 3.16 nM) and inhibiting forskolin-induced cAMP accumulation in CHO cells expressing human D
3 receptors (EC
50 = 2.63 nM). Cariprazine inhibits amphetamine-induced hyperactivity and the conditioned avoidance response in rats (ED
50s = 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.
References
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).
