化学信息：
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化学名
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7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one
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简称
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Brexpiprazole
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别名
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OPC-34712, Rexulti, GTPL7672
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中文名
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依匹唑派
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化学式
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C25H27N3O2S
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分子量
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433.57
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CAS号
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913611-97-9
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO24mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.15ml DMSO，或者每4.34mg加入1ml DMSO，配制成10mM溶液。SD9563-10mM用DMSO配制。
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生物信息：
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产品描述
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Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors.
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信号通路
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Neuronal Signaling; GPCR & G Protein
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靶点
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5-HT1A
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human noradrenergic α1B
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Dopamine D2L
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5-HT2A receptors
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α2C receptors
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IC50
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0.12nM(Ki)
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0.17nM(Ki)
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0.3nM(Ki)
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0.47nM(Ki)
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0.59nM(Ki)
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体外研究
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Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12nM) and dopamine D2L (Ki=0.3nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17nM) and α2Creceptors (Ki=0.59nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiatedngF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth.
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体内研究
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Brexpiprazole is able to ameliorate PCP-191 induced cognitive deficits in mice, via 5-HT1A receptors.
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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PC12 cells
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浓度
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0.001，0.01，0.1或1.0μM
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处理时间
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4 days
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方法
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2.5ng/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 withngF (2.5ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0μM). Four days after incubation withngF (2.5ng/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.
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动物实验
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动物模型
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Male ICR mice
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配制
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0.5% methylcellulose
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剂量
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0.3, 1, or 3mg/kg/day
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给药方式
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oral administration
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参考文献：
1. Ishima T, et al. Eur Neuropsychopharmacol. 2015, 25(4):505-511.
2. Yoshimi N, et al. Pharmacol Biochem Behav. 2014, 124:245-249.
包装清单：
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产品编号
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产品名称
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包装
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SD9563-10mM
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Brexpiprazole (Dopamine Receptor激动剂)
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10mM×0.2ml
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SD9563-5mg
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Brexpiprazole (Dopamine Receptor激动剂)
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5mg
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SD9563-25mg
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Brexpiprazole (Dopamine Receptor激动剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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