| CAS NO: | 913611-97-9 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 433.57 |
| Cas No. | 913611-97-9 |
| Formula | C25H27N3O2S |
| Solubility | ≥21.68 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one |
| Canonical SMILES | C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C5C=CSC5=CC=C4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Brexpiprazole是一种有效的5-HT2A\α1B-和α2C-肾上腺素能受体拮抗剂,同时也是血清素1A(5-HT1A)与D2受体的部分激动剂[1].
5-HT1A受体属于G蛋白偶联受体,可以结合内源性神经递质血清素5-HT以介导抑制性神经传递.D2受体也属G蛋白偶联受体,能够抑制腺苷酸环化酶活性.
在克隆受体系统中,Brexpiprazole对h5-HT1A和hD2受体具有部分激动效应,同时有效地拮抗h5-HT2A受体和hα1B/2C肾上腺素能受体[2].在PC12细胞中,Brexpiprazole作用于5-HT1A受体和5-HT2A受体,从而呈浓度依赖性地增加具有神经突的细胞数量[3].
在Dizocilpine诱导的社会认知障碍小鼠模型中,Brexpiprazole(0.01\0.03和0.1 mg/kg,口服)显著改善认知障碍,对未经处理的对照组小鼠则没有影响.Brexpiprazole有望用于治疗精神疾病患者的社会认知障碍[1].
参考文献：
[1]. Noriko Yoshimi, Takashi Futamura, Kenji Hashimoto. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. European Neuropsychopharmacology, http://dx.doi.org/10.1016/j.euroneuro.2014.12.014
[2]. Maeda K, Sugino H, Akazawa H et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. journal of pharmacology and experimental therapeutics, 2014 Sep;350(3):589-604.
[3]. Tamaki Ishima, Takashi Futamura, Yuta Ohgi et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin–dopamine activity modulator: A role for serotonin 5-HT1A and 5-HT2A receptors. European Neuropsychopharmacology, http://dx.doi.org/10.1016/j.euroneuro.2015.01.014
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