2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor Adrenergic Receptor
  4. Brexpiprazole hydrochloride

Brexpiprazole hydrochloride  (Synonyms: OPC-34712 hydrochloride)

Cat. No.: HY-15780A
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Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).

For research use only. We do not sell to patients.

CAS No. : 913612-38-1

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Brexpiprazole hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Brexpiprazole hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279.  [Abstract]

    To evaluate the effect of the new APD Brexpiprazole (Bre) on glycolipid metabolism during 28 days, rats were randomly divided into four groups, with six female and six male rats in each group: (1) the vehicle group, rats received a blank sweet cookie dough pellet; (2) the Ola group, rats were treated with Ola (1.0 mg/kg); (3) the Ari group, rats were treated with Ari (1.0 mg/kg); (4) the Bre group, rats were treated with Bre (0.5 mg/kg).

    Brexpiprazole hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279.  [Abstract]

    The rats treated with Ola, Ari, or Brexpiprazole (Bre, 0.5 mg/kg) had different degrees of weight gain.

    Brexpiprazole hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279.  [Abstract]

    The rats' FBG was elevated obviously after 3 weeks administration of Ola or Brexpiprazole (Bre, 0.5 mg/kg), while the significant increase of FBG in Ari group only appeared at the 4th week.

    Brexpiprazole hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279.  [Abstract]

    Both the GLP1 expressions in pancreas and small intestine were restrained by Ola or Brexpiprazole (Bre) and a similar effect was observed in GLP1 gene proglucagon (Gcg) by qPCR analysis.

    Brexpiprazole hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279.  [Abstract]

    The pancreas H&E staining exhibited clear and well-organized structure of islets in the vehicle and Ari group rats, but abnormal histological changes such as vacuolization and islet size reduction were detected in both Ola and Brexpiprazole (Bre) groups.

    Brexpiprazole hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279.  [Abstract]

    From the liver H&E staining, we could clearly see the vacuolization in Bre treated rats.

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    Description

    Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2].

    IC50 & Target

    5-HT1A Receptor

     

    5-HT2A Receptor

     

    5-HT1A Receptor

    0.12 nM (Ki)

    5-HT2A Receptor

    0.47 nM (Ki)

    D2L Receptor

    0.3 nM (Ki)

    human noradrenergic α1B

    0.17 nM (Ki)

    human noradrenergic α2C

    0.59 nM (Ki)

    In Vitro

    Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Brexpiprazole hydrochloride Related Antibodies
    In Vivo

    Brexpiprazole (0-0.1 mg/kg; p.o.; once) improves social recognition deficits in mice[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits[2]
    Dosage: 0.01, 0.03 and 0.1 mg/kg
    Administration: Oral administration, once
    Result: Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.
    Clinical Trial
    Formula

    C25H28ClN3O2S
    CAS No.
    SMILES

    O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1.[H]Cl.[x]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Brexpiprazole hydrochloride Related Classifications

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Brexpiprazole913612-38-1OPC-34712OPC34712OPC 347125-HT ReceptorDopamine ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorPC12orally activerecognition deficitsneurite outgrowthantipsychoticInhibitorinhibitorinhibit

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