CAS |
913611-97-9 |
Chinese Name |
依匹唑派 |
English Name |
Brexpiprazole |
Synonyms |
OPC-34712 |
Molecular Formula |
C25H27N3O2S |
Molecular Weight |
433.57 |
Solubility |
Soluble in DMSO ≥2mg/mL(Need ultrasonic) |
Purity |
≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 811-628-7 |
MDL |
MFCD27987920 |
SMILES |
O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1 |
Target Point |
5-HT Receptor,Dopamine Receptor |
Passage |
Neuronal Signaling;GPCR & G Protein |
Background |
It is a novel partial agonist of dopamine receptor D2 and serotonin 1A receptor. |
Biological Activity |
Brexpiprazole (OPC-34712)是一种新型的多巴胺受体D2和5-羟色胺1A受体的部分激动剂,同时也是5-羟色胺2A受体和去甲肾上腺素alpha1B、alpha2C受体的拮抗剂。其对D2L, 5-HT1A, 5-HT2A, α1B受体和 α2C受体的Ki值分别为 0.3, 0.12, 0.47, 0.17 和 0.59 nM。[1] |
IC50 |
5-HT1A(Cell-free assay):0.12nM(Ki);Dopamine D2L(Cell-free assay):0.3nM(Ki);5-HT2A receptors(Cell-free assay):0.47nM(Ki)[1] |
In Vitro |
Brexpiprazole是一种有效的人5-羟色胺 5-HT1A(Ki=0.12 nM)和多巴胺受体D2L(Ki=0.3 nM)的部分激活剂。还是5-HT2A受体的拮抗剂(Ki=0.47 nM)。它对人去甲肾上腺素受体α1B(Ki=0.17 nM)和α2C(Ki=0.59 nM)也有拮抗活性。此外,Brexpiprazole对人D3、5-HT2B、5-HT7、α1A和α1D肾上腺素能受体具有中等亲和力。在PC12细胞中,它能增强NGF引起的神经突增生、增强fluoxetine对神经突增生的作用[1]。 |
In Vivo |
Brexpiprazole在小鼠中通过5-HT1A受体,可改善由PCP-191引起的认知障碍[2]。 |
Cell Experiment |
将细胞接种于细胞板后24小时,将培养基更换为DMEM培养基,包含0.5% FBS和1%青霉素-链霉素以及2.5 ng/ml神经生长因子,加入不同浓度的brexpiprazole(0,0.001,0.01,0.1 or 1.0 μM)。4天后,进行形态测定分析。[1] |
Animal Experiment |
Animal Models: ICR雄性小鼠; Dosages: 0.3,1或3 mg/kg/day; Administration: 口服[2] |
Data Literature Source |
[1] Ishima T,et al. Eur Neuropsychopharmacol. 2015,25(4):505-511. [2] Yoshimi N,et al. Pharmacol Biochem Behav. 2014,124:245-2 |
Unit |
Bottle |
Specification |
5mg 10mg |