化学信息：
| 化学名 | 7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one |
|
| 简称 | Brexpiprazole | |
| 别名 |
OPC-34712, Rexulti, GTPL7672 |
|
| 中文名 | 依匹唑派 | |
| 化学式 | C25H27N3O2S | |
| 分子量 | 433.57 | |
| CAS号 | 913611-97-9 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO24mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 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。 |
生物信息：
| 产品描述 | 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. | ||||
| 信号通路 | Neuronal Signaling; GPCR & G Protein | ||||
| 靶点 | 5-HT1A | human noradrenergic α1B | Dopamine D2L | 5-HT2A receptors | α2C receptors |
| IC50 | 0.12nM(Ki) | 0.17nM(Ki) | 0.3nM(Ki) | 0.47nM(Ki) | 0.59nM(Ki) |
| 体外研究 | 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. | ||||
| 体内研究 | Brexpiprazole is able to ameliorate PCP-191 induced cognitive deficits in mice, via 5-HT1A receptors. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
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)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | PC12 cells |
| 浓度 | 0.001，0.01，0.1或1.0μM |
| 处理时间 | 4 days |
| 方法 | 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. |
| 动物实验 | |
| 动物模型 | Male ICR mice |
| 配制 | 0.5% methylcellulose |
| 剂量 | 0.3, 1, or 3mg/kg/day |
| 给药方式 | oral administration |
| 产品编号 | 产品名称 | 包装 |
| SD9563-10mM | Brexpiprazole (Dopamine Receptor激动剂) | 10mM×0.2ml |
| SD9563-5mg | Brexpiprazole (Dopamine Receptor激动剂) | 5mg |
| SD9563-25mg | Brexpiprazole (Dopamine Receptor激动剂) | 25mg |
| — | 说明书 | 1份 |
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。
