Brexpiprazole

SKU: orb1305739

Description

Brexpiprazole is a small molecule acting as a partial agonist at human serotonin 5-HT1A and dopamine D2 receptors. It is widely used in preclinical research to investigate neuropsychiatric disorders, including schizophrenia and depression, through both in vitro binding assays and in vivo behavioral models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 913611-97-9
• MW: 433.57
• Purity: 99.96%
• Formula: C₂₅H₂₇N₃O₂S
• SMILES: C(CCCOC=1C=C2C(=CC1)C=CC(=O)N2)N3CCN(C4=C5C(SC=C5)=CC=C4)CC3
• Target: Dopamine Receptor,Adrenergic Receptor,5-HT Receptor
• Solubility: DMSO:21 mg/mL (48.44 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Noradrenaline α1B (human):0.17 nM(Ki)|D2L:0.3 nM(Ki)|5-HT1A:0.12 nM(Ki)|5-HT2A receptor:0.47 nM(Ki)|α2C-adrenoceptor:0.59 nM(Ki)
• In Vivo:
  Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors.
• 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.
• Cell Research:
  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. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Serotonin Receptor, recognition deficits, α1B-adrenergic receptor, α2C receptors, antipsychotic, 5-hydroxytryptamine Receptor, 5HTReceptor, 5-HT2A, 5-HT1A, 5HT Receptor, 5-HT Receptor, AdrenergicReceptor, Adrenergic Receptor, Brexpiprazole, Beta Receptor, DopamineReceptor, Dopamine Receptor, Dopamine, D2L, PC12, OPC34712, OPC-34712, OPC 34712, orally active, neurite outgrowth, inhibit, Inhibitor

Compound Identifiers

PubChem CID

11978813