Cariprazine - CAS 839712-12-8
Catalog number:
B0084-459781
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H32Cl2N4O
Molecular Weight:
427.41
COA:
Inquire
Targets:
5-HT Receptor | Dopamine Receptor
Description:
Cariprazine is an orally active D2/D3 dopamine receptor antagonist 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. It is used as an antipsychotic drug candidate for the potential treatment of schizophrenia, bipolar mania and depression. It has also been used as a potential adjunct in treatment-resistant major depressive disorder. It 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) in vitro. It could reduce the rewarding effect of cocaine and attenuated relapse to cocaine seeking with half maximal effective dose values of 0.2, 4.2, and 0.17 mg/kg, respectively. It was developed by Gedeon Richter and received FDA approval on September 17, 2015 and is currently owned by Gedeon Richter and Actavis. It is in phase III clinical trials in patients with schizophrenia and in patients with bipolar disorder.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-459781 25 mg $298 In stock
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Purity:
>98%
Appearance:
White to off-white Solid
Synonyms:
Urea, N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N -diMethyl-;N'-[trans-4-[2-[4-(2,3-Dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea;RGH 188;3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea;Vraylar
Solubility:
10 mM in DMSO ; water:1000 mg/ml
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Cariprazine is used as an antipsychotic drug candidate for the potential treatment of schizophrenia, bipolar mania and depression. It has also been used as a potential adjunct in treatment-resistant major depressive disorder.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams-Kilos
Boiling Point:
600.1±55.0 °C | Condition: Press: 760 Torr
Density:
1.24±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
KPWSJANDNDDRMB-UHFFFAOYSA-N
InChI:
InChI=1S/C21H32Cl2N4O/c1-25(2)21(28)24-17-8-6-16(7-9-17)10-11-26-12-14-27(15-13-26)19-5-3-4-18(22)20(19)23/h3-5,16-17H,6-15H2,1-2H3,(H,24,28)
Canonical SMILES:
CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
Current Developer:
Cariprazine was developed by Gedeon Richter and received FDA approval on September 17, 2015. It is currently owned by Gedeon Richter and Actavis. It is in phase III clinical trials in patients with schizophrenia and in patients with bipolar disorder.
1.Cariprazine (RGH-188), a D3-preferring dopamine D3/D2 receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats
V. Román & I. Gyertyán & K. Sághy & B. Kiss & Zs. Szombathelyi. Psychopharmacology (2013) 226:285–293
Abuse of drugs, such as cocaine, is a frequent comorbidity in psychiatric disorders and is associated with greater morbidity, impairment, and mortality (Drake and Mueser 2000; Schmidt et al. 2011). Because of the huge burden it imposes on psychiatric patients, effective treatment of drug abuse is a high priority. Beyond psychotherapeutic interventions, treatment options are limited; specific and approved pharmacological treatments do not currently exist for cocaine dependence or relapse. Various dopamine receptor ligands, agonists, antagonists, and partial agonists have been intensely investigated in both preclinical settings and human laboratory studies to investigate their potential anti-abuse effect (for review, see Haney and Spealman 2008). Cariprazine is a D3-preferring dopamine D3/D2 receptor partial agonist (Kiss et al. 2010) that has shown efficacy in animal models of psychosis (Gyertyán et al. 2011) and in the treatment of schizophrenia (Bose et al. 2010) and acute mania (Knesevich et al. 2009). The aim of the present study was to determine whether cariprazine shows anti-abuse efficacy in animal models of cocaine dependence.
2.Newer antipsychotics and upcoming molecules for schizophrenia
Melvin George & Radhika Amrutheshwar & Ravi Philip Rajkumar & Shivanand Kattimani & Steven Aibor Dkhar. Eur J Clin Pharmacol (2013) 69:1497–1509
Cariprazine, is a novel antipsychotic which is currently in the pipeline for the treatment of schizophrenia and bipolar disorder. It has a unique receptor binding profile with preferential affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor. Located in limbic areas, ventral striatum and the thalamus, D3 dopamine receptors are shown to be involved in modulating memory function, speech, and attention in schizophrenia. Cariprazine is a novel antipsychotic drug candidate that exhibits partial agonism at D2/D3 receptors. The clinical effects of cariprazine are possibly related to the D3 and D2 receptors, with minimal 5-HT1A-related effects at therapeutic dose levels since the occupancy at 5HT1A receptor sites is only 18 %. These findings have been confirmed in a PET study performed in monkeys where cariprazine in increasing doses showed maximal occupancy of D2/D3 receptors. However the radioligands used in this study could not differentiate the subtype selectivity among dopamine receptors. In another study that was carried out in male subjects with schizophrenia, D2 receptor occupancy was observed to be 69 % in the caudate nucleus and nucleus accumbens and 75 % in the putamen when cariprazine was given at a dose of 1.5 mg/d. Maximal occupancy of 90 % was seen only when the dose was increased to 3 mg/day.
3.The Impact of Psychoactive Drugs on Seizures and Antiepileptic Drugs
Mitra Habibi & Felecia Hart & Jacquelyn Bainbridge. Curr Neurol Neurosci Rep (2016) 16: 71
Several second-generation antipsychotics are major or minor substrates of CYP3A4 and are subject to significant interactions with AEDs that are substrates, inhibitors, or inducers of CYP3A4. Aripiprazole, brexpiprazole, cariprazine, lurasidone, and quetiapine are all major substrates of CYP3A4, and asenapine, clozapine, iloperidone, risperidone, and ziprasidone are all minor substrates. The drug concentrations of these antipsychotics will be decreased by the CYP3A4-inducing AEDs; carbamazepine, phenytoin, oxcarbazepine, rufinamide, eslicarbazepine, phenobarbital, and clobazam.
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CAS 839712-12-8 Cariprazine

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