Serotonin (5-HT) is a neurotransmitter that plays an important physiological role in the human body. Specifically, serotonin is the primary therapeutic target for many mental and neurological disorders associated with decreased levels of central nervous system and plasma serotonin. Besides, the 5-hydroxytryptamine-1A (5-HT1A) receptor is a rich postsynaptic 5-HT receptor (heteroreceptor) that participates in the regulation of emotions, emotions, and stress responses. And it is the main somatic dendritic autoreceptor that negatively regulates the activity of 5-HT neurons. Moreover, dopamine controls various physiological functions in the brain and periphery by acting on its receptors D1, D2, D3, D4, and D5. Furthermore, dopamine receptors are G protein coupled receptors that participate in the regulation of motor activity and various neurological diseases, such as schizophrenia and Parkinson’s disease (PD). There is a serotonin-dopamine activity modulator, Brexpiprazole.

Brexpiprazole is a Serotonin-Dopamine Activity Modulator for Neurological Disease and Cancer Research.

First of all, Brexpiprazole (OPC-34712) is an atypical orally active antipsychotic agent. Meanwhile, Brexpiprazole is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Nonetheless, Brexpiprazole shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).

In the second place, Brexpiprazole with 0-1.0 μM potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells. Importantly, Brexpiprazole with 0-0.1 mg/kg; by p.o. once) improves social recognition deficits in mice.

All in all, Brexpiprazole is a serotonin-dopamine activity modulator for veurological disease and cancer research.


[1] Ishima T, et al. Eur Neuropsychopharmacol. 2015 Apr;25(4):505-11.