Brexpiprazole

• CAT Number: A000061
• CAS Number: 913611-97-9
• Molecular Formula: C25H27N3O2S
• Molecular Weight: 433.6
• Purity: ≥95%
• Target: Dopamine Receptor
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• InChI: InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)
• InChIKey: ZKIAIYBUSXZPLP-UHFFFAOYSA-N
• SMILES: O=C1C=CC2=C(C=C(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)C=C2)N1

Brexpiprazole, also known as OPC-34712, is a novel D2 dopamine partial agonist called serotonin-dopamine activity modulator (SDAM) approved for the treatment of schizophrenia, and as an adjunctive treatment for depression. Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD). Brexpiprazole was approved on 7/10/2015.

Reference

1:Corrigendum to /Efficacy of brexpiprazole in patients with acute schizophrenia: Review of three randomized, double-blind, placebo-controlled studies/ [Schizophr. Res. 174 (2016) 82-92]. Correll CU, Skuban A, Hobart M, Ouyang J, Weiller E, Weiss C, Kane JM.Schizophr Res. 2017 Mar 25. pii: S0920-9964(17)30120-2. doi: 10.1016/j.schres.2017.02.030. [Epub ahead of print] No abstract available. PMID: 28351543
2:Clinical role of brexpiprazole in depression and schizophrenia. Parikh NB, Robinson DM, Clayton AH.Ther Clin Risk Manag. 2017 Mar 10;13:299-306. doi: 10.2147/TCRM.S94060. eCollection 2017. Review. PMID: 28331332 Free PMC Article
3:Brexpiprazole. Markovic M, Gallipani A, Patel KH, Maroney M.Ann Pharmacother. 2017 Apr;51(4):315-322. doi: 10.1177/1060028016678262. Epub 2016 Dec 15. PMID: 28228056
4:Efficacy of Brexpiprazole as Adjunctive Treatment in Major Depressive Disorder With Irritability: Post Hoc Analysis of 2 Pivotal Clinical Studies. Fava M, Weiller E, Zhang P, Weiss C.J Clin Psychopharmacol. 2017 Apr;37(2):276-278. doi: 10.1097/JCP.0000000000000678. No abstract available. PMID: 28195853 Free PMC Article
5:The novel antipsychotic drug brexpiprazole, alone and in combination with escitalopram, facilitates prefrontal glutamatergic transmission via a dopamine D1 receptor-dependent mechanism. Björkholm C, Marcus MM, Konradsson-Geuken Å, Jardemark K, Svensson TH.Eur Neuropsychopharmacol. 2017 Apr;27(4):411-417. doi: 10.1016/j.euroneuro.2017.01.014. Epub 2017 Feb 9. PMID: 28190661
6:Brexpiprazole reduces hyperactivity, impulsivity, and risk-preference behavior in mice with dopamine transporter knockdown-a model of mania. Milienne-Petiot M, Geyer MA, Arnt J, Young JW.Psychopharmacology (Berl). 2017 Mar;234(6):1017-1028. doi: 10.1007/s00213-017-4543-7. Epub 2017 Feb 3. PMID: 28160035
7:Brexpiprazole and cariprazine: distinguishing two new atypical antipsychotics from the original dopamine stabilizer aripiprazole. Frankel JS, Schwartz TL.Ther Adv Psychopharmacol. 2017 Jan;7(1):29-41. doi: 10.1177/2045125316672136. Epub 2016 Oct 17. Review. PMID: 28101322 Free PMC Article
8:Involvement of presynaptic 5-HT1A receptors in the low propensity of brexpiprazole to induce extrapyramidal side effects in rats. Mombereau C, Arnt J, Mørk A.Pharmacol Biochem Behav. 2017 Feb;153:141-146. doi: 10.1016/j.pbb.2016.12.015. Epub 2017 Jan 3. PMID: 28057524
9:Brexpiprazole for the treatment of schizophrenia. Hsu WY, Lane HY, Lin CH.Expert Opin Pharmacother. 2017 Feb;18(2):217-223. doi: 10.1080/14656566.2016.1274972. Epub 2017 Jan 16. Review. PMID: 27997809
10:Adjunctive treatment of brexpiprazole with fluoxetine shows a rapid antidepressant effect in social defeat stress model: Role of BDNF-TrkB signaling. Ma M, Ren Q, Yang C, Zhang JC, Yao W, Dong C, Ohgi Y, Futamura T, Hashimoto K.Sci Rep. 2016 Dec 19;6:39209. doi: 10.1038/srep39209. PMID: 27991542 Free PMC Article