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REXULTI has high binding affinity to 3 neurotransmitter systems: norepinephrine, serotonin, and dopamine
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Pharmacodynamic profile—binding affinities across neurotransmitter systems1,a
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Norepinephrine, serotonin, and dopamine modulate each other's activity2
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The mechanism of action of brexpiprazole is unknown. However, the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors.
aThe binding affinity of brexpiprazole was determined in vitro in cells overexpressing human receptors and is expressed as an nM concentration with lower values representing higher affinity. High binding affinity Ki <1 nM.1
Ki, binding affinity; nM, nanomolar.
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Continue exploring REXULTI
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Please see FULL PRESCRIBING INFORMATION, including BOXED WARNING.
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References: 1. Maeda K, Sugino H, Akazawa H, et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014;350(3):589-604. 2. Mansari M, Guiard BP, Chernoloz O, et al. Relevance of norepinephrine-dopamine interactions in the treatment of major depressive disorder. CNS Neurosci Ther. 2010;16(3):e1-e17.
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