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- Brexpiprazole 913611-97-9

- Brexpiprazole 913611-97-9
Brexpiprazole 913611-97-9
产品描述 描述 Brexpiprazole is a novel D2 dopamine partial agonist.
纯度 99%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 OPC-34712;OPC34712可溶性/溶解性 DMSO :24mg/ml(55.35 mM)生物活性 靶点 5-HT ReceptorIn vitro(体外研究) Brexpiprazole, a novel serotonin-dopamine activity modulator: A role for serotonin 5-HT1A and 5-HT2A receptors. Brexpiprazole also shows potent antagonist activity at human nor adrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM). Brexpiprazole significantly potentiates nerve growth factor (NGF)-induced neurite outgrowth in PC12 cells, in a concentration dependent manner. Brexpiprazole (1 μM) increases the number of cells with neurites in PC12 cells. Treatment with Brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM) in conjunction with NGF (2.5 ng/mL) increases the number of cells with neurites, in a concentration-dependent manner.In vivo(体内研究) Brexpiprazole (0.01, 0.03, 0.1 mg/kg, p.o.) significantly ameliorates dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior. In addition, Brexpiprazole alone has no effect on social recognition in untreated controlmice. By contrast, neither Risperidone(0.03 mg/kg, p.o.) nor Olanzapine (0.03 mg/kg, p.o.) alters Dizocilpine induced social recognition deficits. Finally,the effect of Brexpiprazole on Dizocilpine-induced social recognition deficits is antagonized by WAY-100,635. These results suggest that Brexpiprazole can improve Dizocilpine-induced social recognition deficits via 5-HT1A receptor activation in mice.参考文献 参考文献 1. Zajdel P, et al. Future Med Chem, 2014. 6(1): p. 57-75.
研究领域 研究领域 MetabolismTypes of diseaseObesityNeuroscienceProcessesNeuroscienceNeurology processMetabolismNeuroscienceNeurotransmissionReceptors / ChannelsGPCRSerotonin ReceptorsSignal TransductionSignaling PathwayG Protein SignalingGPCRDrug DiscoverySmall Molecule DrugLead Compound DiscoveryBrexpiprazole 913611-97-9温馨提示:本产品仅作科研实验使用,不支持临床等研究
