Cariprazine HCl
Cariprazine, also known as RGH-188 and MP-214, is an antipsychotic drug received FDA approval on September 17, 2015. Cariprazine acts as a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor. Action on the dopaminergic systems makes it also potentially useful as an add-on therapy in major depressive disorder. Cariprazine is approved for schizophrenia and bipolar disorder. It has also been investigated as a potential adjunct in treatment-resistant major depressive disorder.
For research use only. We do not sell to patients.
Chemical Information
| Name | Cariprazine HCl |
|---|---|
| Iupac Chemical Name | 3-((1r,4r)-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea hydrochloride |
| Synonyms | RGH-188; RGH188; RGH 188; MP-214; MP 214; MP214; Cariprazine. trade name Vraylar |
| Molecular Formula | C21H33Cl3N4O |
| Molecular Weight | 463.872 |
| Smile | O=C(N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1)N(C)C.[H]Cl |
| InChiKey | GPPJWWMREQHLQT-BHQIMSFRSA-N |
| InChi | InChI=1S/C21H32Cl2N4O.ClH/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);1H/t16-,17-; |
| CAS Number | 839712-12-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548595/ PubMed PMID: 31643910.
2: Citrome L. Cariprazine for bipolar depression: What is the number needed to treat, number needed to harm and likelihood to be helped or harmed? Int J Clin Pract. 2019 Oct;73(10):e13397. doi: 10.1111/ijcp.13397. Epub 2019 Aug 19. Review. PubMed PMID: 31355510.
3: Corponi F, Fabbri C, Bitter I, Montgomery S, Vieta E, Kasper S, Pallanti S, Serretti A. Novel antipsychotics specificity profile: A clinically oriented review of lurasidone, brexpiprazole, cariprazine and lumateperone. Eur Neuropsychopharmacol. 2019 Sep;29(9):971-985. doi: 10.1016/j.euroneuro.2019.06.008. Epub 2019 Jun 27. Review. PubMed PMID: 31255396.
4: Misiak B, Bieńkowski P, Samochowiec J. Cariprazine - a novel antipsychotic drug and its place in the treatment of schizophrenia. Psychiatr Pol. 2018 Dec 29;52(6):971-981. doi: 10.12740/PP/OnlineFirst/80710. Epub 2018 Dec 29. Review. English, Polish. PubMed PMID: 30659560.
5: Citrome L. Cariprazine for acute and maintenance treatment of adults with schizophrenia: an evidence-based review and place in therapy. Neuropsychiatr Dis Treat. 2018 Oct 5;14:2563-2577. doi: 10.2147/NDT.S159704. eCollection 2018. Review. PubMed PMID: 30323605; PubMed Central PMCID: PMC6179724.
6: Mazza M, Marano G, Traversi G, Carocci V, Romano B, Janiri L. Cariprazine in Bipolar Depression and Mania: State of the Art. CNS Neurol Disord Drug Targets. 2018;17(10):723-727. doi: 10.2174/1871527317666180828120256. Review. PubMed PMID: 30152291.
7: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500757/ PubMed PMID: 29999816.
8: Wesołowska A, Partyka A, Jastrzębska-Więsek M, Kołaczkowski M. The preclinical discovery and development of cariprazine for the treatment of schizophrenia. Expert Opin Drug Discov. 2018 Aug;13(8):779-790. doi: 10.1080/17460441.2018.1471057. Epub 2018 May 3. Review. PubMed PMID: 29722587.
9: Zhao MJ, Qin B, Wang JB, Zhang YP, Zhao JT, Mao YG, Zhang XY, Zhang RL. Efficacy and Acceptability of Cariprazine in Acute Exacerbation of Schizophrenia: Meta-Analysis of Randomized Placebo-Controlled Trials. J Clin Psychopharmacol. 2018 Feb;38(1):55-59. doi: 10.1097/JCP.0000000000000834. Review. PubMed PMID: 29257786.
10: Durgam S, Earley W, Lu K, Németh G, Laszlovszky I, Volk S, Litman RE. Global improvement with cariprazine in the treatment of bipolar I disorder and schizophrenia: A pooled post hoc analysis. Int J Clin Pract. 2017 Dec;71(12). doi: 10.1111/ijcp.13037. Epub 2017 Nov 9. Review. PubMed PMID: 29119668; PubMed Central PMCID: PMC5765496.
11: Garnock-Jones KP. Cariprazine: A Review in Schizophrenia. CNS Drugs. 2017 Jun;31(6):513-525. doi: 10.1007/s40263-017-0442-z. Review. PubMed PMID: 28560619.
12: Frankel JS, Schwartz TL. Brexpiprazole and cariprazine: distinguishing two new atypical antipsychotics from the original dopamine stabilizer aripiprazole. Ther Adv Psychopharmacol. 2017 Jan;7(1):29-41. doi: 10.1177/2045125316672136. Epub 2016 Oct 17. Review. PubMed PMID: 28101322; PubMed Central PMCID: PMC5228714.
13: Scarff JR. Cariprazine for Schizophrenia and Bipolar Disorder. Innov Clin Neurosci. 2016 Oct 1;13(9-10):49-52. eCollection 2016 Sep-Oct. Review. PubMed PMID: 27975000; PubMed Central PMCID: PMC5141596.
14: Lao KS, He Y, Wong IC, Besag FM, Chan EW. Tolerability and Safety Profile of Cariprazine in Treating Psychotic Disorders, Bipolar Disorder and Major Depressive Disorder: A Systematic Review with Meta-Analysis of Randomized Controlled Trials. CNS Drugs. 2016 Nov;30(11):1043-1054. Review. PubMed PMID: 27550371.
15: Roberts RJ, Findlay LJ, El-Mallakh PL, El-Mallakh RS. Update on schizophrenia and bipolar disorder: focus on cariprazine. Neuropsychiatr Dis Treat. 2016 Jul 25;12:1837-42. doi: 10.2147/NDT.S97616. eCollection 2016. Review. PubMed PMID: 27524901; PubMed Central PMCID: PMC4966692.
16: Citrome L. Cariprazine for the Treatment of Schizophrenia: A Review of this Dopamine D3-Preferring D3/D2 Receptor Partial Agonist. Clin Schizophr Relat Psychoses. 2016 Summer;10(2):109-19. doi: 10.3371/1935-1232-10.2.109. Review. PubMed PMID: 27440212.
17: De Berardis D, Orsolini L, Iasevoli F, Prinzivalli E, de Bartolomeis A, Serroni N, Mazza M, Valchera A, Fornaro M, Vecchiotti R, Carano A, Sepede G, Vellante F, Matarazzo I, Pompili M, Perna G, Conti C, Segura-García C, Martinotti G, Di Giannantonio M. The Novel Antipsychotic Cariprazine (RGH-188): State-of-the-Art in the Treatment of Psychiatric Disorders. Curr Pharm Des. 2016;22(33):5144-5162. Review. PubMed PMID: 27396597.
18: Cariprazine (Vraylar) for schizophrenia and bipolar I disorder. Med Lett Drugs Ther. 2016 Apr 25;58(1493):51-3. Review. PubMed PMID: 27101209.
19: De Deurwaerdère P. Cariprazine:New dopamine biased agonist for neuropsychiatric disorders. Drugs Today (Barc). 2016 Feb;52(2):97-110. doi: 10.1358/dot.2016.52.2.2461868. Review. PubMed PMID: 27092339.
20: Findlay LJ, El-Mallakh PL, El-Mallakh RS. Cariprazine for the Treatment of Bipolar Disorder. Perspect Psychiatr Care. 2017 Jul;53(3):148-155. doi: 10.1111/ppc.12150. Epub 2016 Apr 5. Review. PubMed PMID: 27059102.
Chemical Structure
