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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]

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