Cariprazine-d6 Property

storage temp. 

Store at -20°C

solubility 

DMSO: soluble

form 

A solid

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

Cariprazine-d6 Chemical Properties,Usage,Production

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 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.

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).