Brexpiprazole (Dopamine激动剂)10mM×0.2ml上海生物网SD9563

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。

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

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