Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.

D2L:0.3 nM(Ki), 5-HT1A:0.12 nM(Ki), Noradrenaline α1B (human):0.17 nM(Ki), 5-HT2A receptor:0.47 nM(Ki), α2C-adrenoceptor:0.59 nM(Ki)

Brexpiprazole是一种在人体5-羟色胺 (5-HT) 5-HT1A (Ki=0.12 nM) 和多巴胺D2L (Ki=0.3 nM) 受体上表现出强有力部分激动剂活性，并在5-HT2A受体上表现出拮抗活性 (Ki=0.47 nM) 的化合物。它同样在人体去甲肾上腺素α1B (Ki=0.17 nM) 和α2C受体 (Ki=0.59 nM) 上显示出强有力的拮抗作用。此外，该化合物对人体D3、5-HT2B和5-HT7受体，以及α1A和α1D肾上腺素受体表现出中等亲和力。Brexpiprazole增强了PC12细胞中NGF诱导的神经突生长。它可以显着增强fluoxetine（或paroxetine）对神经突生长的效果[1]。

Brexpiprazole可通过5-HT1A受体减轻PCP-191在小鼠中引起的认知缺失[2]。

2.5 ng/ml of NGF(nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin with NGF (2.5 ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM). Four days after incubation with NGF (2.5 ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera. (Only for Reference)