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Catalog No.
5-HT2A, α1B-, and α2C-adrenergic receptors antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock
In stock

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Brexpiprazole is a potent antagonist effects on 5-HT2A, α1B-, and α2C-adrenergic receptors and a partial agonist at serotonin 1A (5-HT1A) and D2 receptors. [1]
5-HT1A receptor is a G protein-coupled receptor that can mediates inhibitory neurotransmission by binding the endogenous neurotransmitter serotonin5-HT. And D2 receptor is a G protein-coupled receptor inhibits adenylyl cyclase activity.
In cloned receptor systems, brexpiprazole displayed partial agonist at h5-HT1A and hD2 receptors, and potent antagonism of h5-HT2A receptors and hα1B/2C-adrenoceptors. [2] When tested in PC12 cells, brexpiprazole increased the number of cells with neurites in a concentration-dependent manner through 5-HT1A receptors and 5-HT2A receptors.[3]
In the dizocilpine-induced social recognition deficits mice model, brexpiprazole (0.01, 0.03, 0.1mg/kg,p.o.) significantly ameliorated the recognition deficits, and had no effect on social recognition in untreated control mice. Brexpiprazole may confer a beneficial effect on social cognition deficits in patients with psychiatric disorders. [1]
[1]. Noriko Yoshimi, Takashi Futamura, Kenji Hashimoto. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. European Neuropsychopharmacology,
[2]. Maeda K, Sugino H, Akazawa H et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. journal of pharmacology and experimental therapeutics, 2014 Sep;350(3):589-604.
[3]. Tamaki Ishima, Takashi Futamura, Yuta Ohgi et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin–dopamine activity modulator: A role for serotonin 5-HT1A and 5-HT2A receptors. European Neuropsychopharmacology,

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.913611-97-9
Solubility≥21.68mg/mL in DMSO with gentle warming
Chemical Name7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one
SDFDownload SDF
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

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