Brexpiprazole

Catalog No.S4639 Synonyms: OPC-34712

For research use only.

Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.

Brexpiprazole Chemical Structure

CAS No. 913611-97-9

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Biological Activity

Description Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.
Targets
5-HT1A [1]
(Cell-free assay)
human noradrenergic α1B [1]
(Cell-free assay)
Dopamine D2L [1]
(Cell-free assay)
5-HT2A receptors [1]
(Cell-free assay)
α2C receptors [1]
(Cell-free assay)
0.12 nM(Ki) 0.17 nM(Ki) 0.3 nM(Ki) 0.47 nM(Ki) 0.59 nM(Ki)
In vitro

Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiated NGF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth[1].

In vivo Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors[2].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: PC12 cells
  • Concentrations: 0.001, 0.01, 0.1 or 1.0 μM
  • Incubation Time: 4 days
  • Method: 2.5 ng/ml of NGF(nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin with NGF (2.5 ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM). Four days after incubation with NGF (2.5 ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera.
Animal Research:[2]
  • Animal Models: Male ICR mice
  • Dosages: 0.3, 1, or 3 mg/kg/day
  • Administration: oral administration

Solubility (25°C)

In vitro

DMSO 24 mg/mL
(55.35 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 433.57
Formula

C25H27N3O2S

CAS No. 913611-97-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C5C=CSC5=CC=C4

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03734354 Completed Drug: Brexpiprazole Health Otsuka Beijing Research Institute April 7 2019 Phase 1
NCT02875080 Completed Drug: OPC-34712 Healthy Adult Male Otsuka Pharmaceutical Co. Ltd. September 27 2016 Phase 1
NCT00905307 Completed Drug: OPC-34712|Drug: Placebo|Drug: Aripiprazole Schizophrenia Otsuka Pharmaceutical Development & Commercialization Inc. July 2009 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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