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Cariprazine hydrochloride CAS: 1083076-69-0

Category: Inhibitors
Product Name: Cariprazine hydrochloride
Cat No: I000363
CAS No: 1083076-69-0
Synonyms: 3-(4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea hydrochloride
Molecular Formula: C21H33Cl3N4O
Molecular Weight: 463.87
Solubility: 10 mM in DMSO
Target: Dopamine Receptor
IC50: 0.5 and 0.09 nM (Ki for D2 and D3 receptor respectively); 2.6 and 180 nM (Ki for 5-HT1A and 5-HT2A receptor respectively) [1]
Storage: Store at -20°C
CAS 1083076-69-0,Cariprazine hydrochloride
  • Description

Cariprazine Hcl(RGH188) is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptors and moderate affinity to serotonin 5-HT(1A) receptors.
IC50 Value: 0.5 and 0.09 nM (Ki for D2 and D3 receptor respectively); 2.6 and 180 nM (Ki for 5-HT1A and 5-HT2A receptor respectively) [1]
Target: D2;D3; 5-HT1A; 5-HT2A
in vitro: Cariprazine had lower affinity at human and rat hippocampal 5-HT(1A) receptors (pK(i) 8.59 and 8.34, respectively) and demonstrated low intrinsic efficacy.Cariprazine displayed low affinity at human 5-HT(2A) receptors (pK(i) 7.73). Moderate or low affinity for histamine H(1) and 5-HT(2C) receptors (pK(i) 7.63 and 6.87, respectively) suggest cariprazine's reduced propensity for adverse events related to these receptors [2].
in vivo: Doses ≥ 1.5 mg/d yielded 69 - 75% D2/D3 receptor occupancy as measured in positron emission tomography scans. Mean half-life for cariprazine was 2 - 5 d over a dose range of 1.5 - 12.5 mg [3]. Cariprazine, as well as aripiprazole and bifeprunox, were able to reduce the rewarding effect of cocaine (minimum effective doses were 0.17, 1, and 0.1 mg/kg, respectively) and attenuated relapse to cocaine seeking with half maximal effective dose [ED] values of 0.2, 4.2, and 0.17 mg/kg, respectively [4].
Toxicity: In the fixed-dose study of cariprazine that tested 1.5, 3.0, and 4.5 mg/day, the most commonly encountered adverse events were insomnia, extrapyramidal disorder, sedation, akathisia, nausea, dizziness, vomiting, anxiety, and constipation [5].
Clinical trial: Cariprazine is in phase III clinical trials in patients with schizophrenia and in patients with bipolar disorder.

  • References

[1]. Seneca N, et al. Occupancy of dopamine D? and D? and serotonin 5-HT?A receptors by the novel antipsychotic drug candidate,cariprazine (RGH-188), in monkey brain measured using positron emission tomography. Psychopharmacology (Berl). 2011 Dec;218(3):579-87.
[2]. Kiss B, et al. Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. J Pharmacol Exp Ther. 2010 Apr;333(1):328-40.
[3]. Citrome L. Cariprazine : chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206.
[4]. Román V, et al. Cariprazine (RGH-188), a D?-preferring dopamine D?/D? receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats. Psychopharmacology (Berl). 2013 Mar;226(2):285-93.
[5]. Citrome L. Cariprazine in schizophrenia: clinical efficacy, tolerability, and place in therapy. Adv Ther. 2013 Feb;30(2):114-26.

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