913612-38-1

Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2].

5-HT_1A Receptor: 0.12 nM (Ki); 5-HT_2A Receptor: 0.47 nM (Ki); D_2L Receptor: 0.3 nM (Ki); human noradrenergic α_1B: 0.17 nM (Ki); human noradrenergic α_2C: 0.59 nM (Ki)

[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. DOI:10.1016/j.euroneuro.2015.01.014
[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. DOI:10.1016/j.euroneuro.2014.12.014