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REXULTI® (brexpiprazole) and antidepressants both interact with some of the same neurotransmitter systems implicated in depression, but in different ways1,2:
Antidepressant treatments that inhibit the reuptake of monoamines include:
REXULTI has binding affinity to 3 neurotransmitter receptor systems
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.3
5-HT, serotonin; D, dopamine; NE, norepinephrine; SNRI, serotonin and norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor.
In addition to serotonin and dopamine, REXULTI has high binding affinity to norepinephrine receptors4
binding affinities across neurotransmitter systems4,a
Serotonin, dopamine, and norepinephrine modulate each other’s activity5
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.4
Ki, binding affinity; nM, nanomolar.
Access a digital brochure detailing the binding profile for REXULTI,
including the pharmacodynamic profile.