Brexpiprazole hydrochloride
Based on 6 publication(s) in Google Scholar
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
- Formula: C25H28ClN3O2S
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) Brexpiprazole hydrochloride
More- Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
- Transl Psychiatry. 2025 Mar 8;15(1):77. [Abstract]
- Eur J Pharmacol. 2021 Nov 15:911:174557. [Abstract]
- Eur J Pharm Sci. 2025 Nov 1:214:107296. [Abstract]
- Pharmacol Rep. 2023 Apr;75(2):266-275. [Abstract]
- Fundam Clin Pharmacol. 2022 Dec;36(6):976-984. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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WB
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IHC
All 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
MoreAll Adrenergic Receptor Isoforms
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Biological Activity
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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) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits[2]
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Dosage:0.01, 0.03 and 0.1 mg/kg
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Administration:Oral administration, once
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Result:Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 913612-38-1
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Formula C25H28ClN3O2S
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SMILES
O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1.[H]Cl.[x]
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Synonyms
OPC-34712 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Brexpiprazole caused glycolipid metabolic disorder by inhibiting GLP1/GLP1R signaling in rats. [Abstract]2021 Aug;42(8):1267-1279. PMID: 33976388
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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Transl Psychiatry
Fine-tuning of dopamine receptor signaling with aripiprazole counteracts ketamine's dissociative action, but not its antidepressant effect. [Abstract]2025 Mar 8;15(1):77. PMID: 40057507 -
Eur J Pharmacol
2021 Nov 15:911:174557. PMID: 34626593 -
Eur J Pharm Sci
Repurposing of FDA-approved drugs by targeting SIRT2 to alleviate inflammatory response and kidney injury. [Abstract]2025 Nov 1:214:107296. PMID: 41022315 -
Pharmacol Rep
Agonistic properties of a series of psychotropic drugs at 5-HT1A receptors in rat and human brain membranes determined by [35S]GTPγS binding assay. [Abstract]2023 Apr;75(2):266-275. PMID: 36637685 -
Fundam Clin Pharmacol
Receptor density influences the recruitment bias of aripiprazole and brexpiprazole at the dopamine D2L receptor. [Abstract]2022 Dec;36(6):976-984. PMID: 35767599
Purity & Documentation
References
[1]. Ishima T, et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin-dopamine activity modulator: a role for serotonin 5-HT1A and 5-HT2A receptors. Eur Neuropsychopharmacol. 2015 Apr;25(4):505-11. [Content Brief]
[2]. Yoshimi N, et al. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. Eur Neuropsychopharmacol. 2015 Mar;25(3):356-64. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Brexpiprazole hydrochloride Related Classifications
HY-15780A Related Classifications
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