Brexpiprazole

• CAT Number: A000061
• CAS Number: 913611-97-9
• Molecular Formula: C25H27N3O2S
• Molecular Weight: 433.60
• Purity: ≥95%
• Synonyms: OPC-34712, OPC 34712, OPC34712
• Target: Neuronal Signaling
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: 7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one
• 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: C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C5C=CSC5=CC=C4

Brexpiprazole（Cat No.:A000061）is an atypical antipsychotic medication with the molecular formula C25H27N3O2S, used primarily to treat schizophrenia and as an adjunctive therapy for major depressive disorder (MDD). It acts as a serotonin-dopamine activity modulator, functioning as a partial agonist at 5-HT1A and D2 receptors, and an antagonist at 5-HT2A and noradrenaline alpha-1B/2C receptors. This balanced receptor profile helps reduce psychotic symptoms while minimizing side effects like extrapyramidal symptoms. Brexpiprazole is administered orally and offers a favorable safety and tolerability profile, making it suitable for long-term management of psychiatric conditions.

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
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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
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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
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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