BrexpiprazoleBrexpiprazole
MedChemExpress (MCE)
HY-15780
913611-97-9
OPC-34712
99.85%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, 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 also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells[1].
Brexpiprazole (0-0.1 mg/kg
p.o.
once) improves social recognition deficits in mice[2].
5-HT1A Receptor 0.12 nM (Ki) 5-HT2A Receptor 0.47 nM (Ki) D2L Receptor 0.3 nM (Ki) human noradrenergic α1B 0.17 nM (Ki) human noradrenergic α2C 0.59 nM (Ki)
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[1]. Ishima T, et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin-dopamine activity modulator: a role for serotonin 5-HT1A and 5-HT2A receptors. Eur Neuropsychopharmacol. 2015 Apr
25(4):505-11. [Content Brief]
[2]. Yoshimi N, et al. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. Eur Neuropsychopharmacol. 2015 Mar
25(3):356-64. [Content Brief]