| Hazard Information | Back Directory | [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 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).2 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).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. | [Uses]
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1]. | [IC 50]
Dopamine D2 Receptor: 0.49 nM (Ki); Dopamine D3 Receptor: 0.085 nM (Ki); 5-HT1A Receptor: 2.6 nM (Ki) | [storage]
Store at -20°C | [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). |
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