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REXULTI® (brexpiprazole) and antidepressants both interact with some of the same neurotransmitter systems implicated in depression, but in different ways1-3:
The activity of these compounds is based on in vitro data. The clinical significance of the in vitro data is unknown. Reuptake inhibitors modulate neurotransmitter activity through different processes than partial agonists and antagonists.4
5-HT, serotonin; D, dopamine; NE, norepinephrine; NDRI, norepinephrine and dopamine reuptake inhibitor; SNRI, serotonin and norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor.
REXULTI has high binding affinity to 3 neurotransmitter systems: norepinephrine, serotonin, and dopamine
Pharmacodynamic profile—binding affinities
across neurotransmitter systems5,a
Norepinephrine, serotonin, and dopamine
modulate each other's activity6
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.5
Ki, binding affinity; nM, nanomolar.
Explore the pharmacodynamics of REXULTI with Dr. Jain
Rakesh Jain, MD, MPH
Department of Psychiatry
Texas Tech University School of Medicine
Access a digital brochure detailing the binding profile for REXULTI,
including the pharmacodynamic profile.