Brexpiprazole - CAS 913611-97-9
Catalog number: B0084-474906
Category: Inhibitor
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Molecular Formula:
C25H27N3O2S
Molecular Weight:
433.58
COA:
Inquire
Targets:
Dopamine Receptor
Description:
Brexpiprazole, a novel atypical antipsychotic drug, is a D2 dopamine partial agonist called serotonin-dopamine activity modulator (SDAM). It is approved for the treatment of schizophrenia, and as an adjunctive treatment for depression. It is a drug candidate useful in treatment and prevention of mental disorders including CNS disorders. It is a close structural analog of aripiprazole and shares some of its pharmacological properties in vitro. It failed Phase II clinical trials for ADHD and was received FDA approval on July 13, 2015. It was developed by Otsuka and Lundbeck. It has been listed.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474906 1 g $199 In stock
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Purity:
> 95%
Appearance:
White Solid
Synonyms:
7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]- 2(1H)-Quinolinone;7-[4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one;Rexulti;OPC-34712; OPC 34712; OPC34712
Solubility:
DMSO: ≥ 48 mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Brexpiprazole is approved for the treatment of schizophrenia, and as an adjunctive treatment for depression. It is a drug candidate useful in treatment and prevention of mental disorders including CNS disorders.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Kilogram to ton
Boiling Point:
675.2±55.0 °C | Condition: Press: 760 Torr
Density:
1.245±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
ZKIAIYBUSXZPLP-UHFFFAOYSA-N
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)
Canonical SMILES:
C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C5C=CSC5=CC=C4
Current Developer:
Brexpiprazole was developed by Otsuka and Lundbeck. It has been listed.
1.Brexpiprazole: a new leaf on the partial dopamine agonist branch.
Hope J;Castle D;Keks NA Australas Psychiatry. 2018 Feb;26(1):92-94. doi: 10.1177/1039856217732473. Epub 2017 Oct 10.
OBJECTIVES: ;Brexpiprazole is a new dopamine partial agonist antipsychotic in the same class as aripiprazole. This paper will briefly review brexpiprazole and compare it with aripiprazole.;CONCLUSIONS: ;Brexpiprazole and aripiprazole are both partial agonists at dopamine D;2;, and serotonin 5-HT;1A; and antagonists at serotonin 5-HT;2A; and noradrenergic α;1B; receptors. However, the two drugs are significantly different in potencies at various receptors; neurochemical profiles predict that brexpiprazole may be comparable with aripiprazole in its antipsychotic efficacy but may cause less akathisia, extrapyramidal side effects (EPS) and activation. In pivotal trials brexpiprazole demonstrated antipsychotic efficacy in short and long-term studies; it was also found to be an effective adjunct in patients with major depression resistant to antidepressants. Akathisia can occur early in treatment with brexpiprazole, as can minor weight gain and prolactin elevation. Indirect data extrapolations from pivotal studies suggest that brexpiprazole and aripiprazole have comparable efficacy but brexpiprazole may cause less akathisia. Like aripiprazole, brexpiprazole has been approved in the USA for use in schizophrenia and antidepressant-resistant depression.
2.Antipsychotic Drug-Induced Somnolence: Incidence, Mechanisms, and Management.
Fang F;Sun H;Wang Z;Ren M;Calabrese JR;Gao K CNS Drugs. 2016 Sep;30(9):845-67. doi: 10.1007/s40263-016-0352-5.
Somnolence is a common side effect of antipsychotics. To assess the incidence of this side effect, we performed a MEDLINE search for randomized, double-blinded, placebo- or active-controlled studies of adult patients treated with antipsychotics for schizophrenia, mania, bipolar depression, or bipolar disorder. We extracted rates of somnolence from original publications and pooled them based on the dose of each antipsychotic in the same psychiatric condition, then estimated the absolute risk increase (ARI) and the number needed to harm (NNH) of an antipsychotic relative to placebo or an active comparator in the same psychiatric condition. According to the ARI in acute schizophrenia, bipolar mania, and bipolar depression, antipsychotics can be classified as high somnolence (clozapine), moderate somnolence (olanzapine, perphenazine, quetiapine, risperidone, ziprasidone), and low somnolence (aripiprazole, asenapine, haloperidol, lurasidone, paliperidone, cariprazine). The risk of somnolence with blonanserin, brexpiprazole, chlorpromazine, iloperidone, sertindole, and zotepine needs further investigation. The rates of somnolence were positively correlated to dose and duration for some antipsychotics, but not for others.
3.The preclinical discovery and development of brexpiprazole for the treatment of major depressive disorder.
Aftab A;Gao K Expert Opin Drug Discov. 2017 Oct;12(10):1067-1081. doi: 10.1080/17460441.2017.1354849. Epub 2017 Jul 18.
Brexpiprazole is the most recently approved second-generation antipsychotic, which is used as adjunctive therapy to antidepressants for treating major depressive disorder (MDD) with inadequate response. Brexpiprazole shares pharmacological similarities with other second-generation antipsychotics, especially aripiprazole. Area covered: This review provides a detailed overview of the pre-clinical studies of brexpiprazole, followed by a summary of its clinical studies, and a comparison with other antipsychotics in MDD. Brexpiprazole is superior to placebo in reducing depressive symptoms of patients who have had an inadequate response to a standard antidepressant treatment. The efficacy of brexpiprazole is comparable to aripiprazole and quetiapine-XR, but brexpiprazole has demonstrated a lower risk for akathisia than aripiprazole and a lower risk for somnolence than quetiapine-XR. Expert opinion: Given that different studies have used different criteria to define 'treatment-resistance' or 'inadequate-response', an accurate comparison of the efficacy and safety of brexpiprazole with other antipsychotics is difficult. Preclinical data supports the premise that the antidepressant-like effects of antipsychotics are mainly due to their ability to modulate/regulate the monoamine system.
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CAS 913611-97-9 Brexpiprazole

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