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Aripiprazole/阿立哌唑 {[allProObj[0].p_purity_real_show]}

货号:A134405 同义名: OPC-14597; OPC 31

Aripiprazole is a multiple-target agent used to treat schizophrenia and bipolar disorder, working as both a silent antagonist and a high-efficacy partial agonist of D2 receptor, as well as works as a partial agonist of 5-HT1A/5-HT2A, 5-HT2 receptor,a potent inverse agonist of 5-HT2B receptor, a functional antagonist of 5-HT7 receptor.

Aripiprazole/阿立哌唑 化学结构 CAS号:129722-12-9
Aripiprazole/阿立哌唑 化学结构
CAS号:129722-12-9
Aripiprazole/阿立哌唑 3D分子结构
CAS号:129722-12-9
Aripiprazole/阿立哌唑 化学结构 CAS号:129722-12-9
Aripiprazole/阿立哌唑 3D分子结构 CAS号:129722-12-9
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Aripiprazole/阿立哌唑 纯度/质量文件 产品仅供科研

货号:A134405 标准纯度: {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

98%
Venlafaxine 99%
Fluvoxamine maleate 99%
Iloperidone 99%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 99%
Fluoxetine HCl 99.5%
Paroxetine HCl AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

95%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

98%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron HCl dihydrate 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Aripiprazole/阿立哌唑 生物活性

描述 Aripiprazole, a partial agonist at dopamine D2 receptors, mainly used as a kind of antipsychotic[3]. In vitro studies, aripiprazole could inhibite the growth of serum-cultured cancer cells and cancer stem cells, induce differentiation and suppress sphere formation while had non-toxic to normal cells[4]. In vivo studies, it was found that long-term administration of aripiprazole could restore DARPP-32 phosphorylation changes in response to sucrose and reinstate the motivational drive to acquire the reward in the progressive ratio task in non food-deprived 9-week old male Sprague-Dawley rats, while wouldn’t restore reactivity to aversive stimuli[5]. Besides this, after administration for 28 days in rats, aripiprazole contributed to the decreases of D2 receptor levels in various regions and 5-HT2A receptors in the MPC, DFC, HIPP-CA1, and HIPP-CA3 regions, as well as the increasing of 5-HT1A receptors in the MPC and DFC, and 5-HT1A receptors in HIPP-CA1 and HIPP-CA3[6].

Aripiprazole/阿立哌唑 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01739127 - Completed - Canada, British Columbia ... 展开 >> BC Mental Health & Addictions Research Institute Vancouver, British Columbia, Canada, V5Z 4H4 收起 <<
NCT00806234 Psychotic Disorders Phase 4 Completed - United States, Maryland ... 展开 >> University of Maryland Baltimore, Maryland, United States, 21201 Johns Hopkins Hospital Baltimore, Maryland, United States, 21205 United States, New York The Zucker Hillside Hospital Glen Oaks, New York, United States, 11004 United States, North Carolina University of North Carolina, Division of Child and Adolescent Psychiatry Chapel Hill, North Carolina, United States, 27599 收起 <<
NCT00895921 Diabetes Phase 4 Completed - United States, California ... 展开 >> VA San Diego Healthcare System San Diego, California, United States, 92161 收起 <<

Aripiprazole/阿立哌唑 参考文献

[1]Shapiro DA, Renock S, et al. Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. Neuropsychopharmacology. 2003 Aug;28(8):1400-11.

[2]Burris KD, Molski TF, et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9.

[4]Suzuki S, Okada M, Kuramoto K, Takeda H, Sakaki H, Watarai H, Sanomachi T, Seino S, Yoshioka T, Kitanaka C. Aripiprazole, an Antipsychotic and Partial Dopamine Agonist, Inhibits Cancer Stem Cells and Reverses Chemoresistance. Anticancer Res. 2016 Oct;36(10):5153-5161. doi: 10.21873/anticanres.11085. PMID: 27798875.

[5]Scheggi S, Pelliccia T, Gambarana C, De Montis MG. Aripiprazole relieves motivational anhedonia in rats. J Affect Disord. 2018 Feb;227:192-197. doi: 10.1016/j.jad.2017.10.032. Epub 2017 Oct 20. PMID: 29100151.

[6]Choi YK, Adham N, Kiss B, Gyertyán I, Tarazi FI. Long-term effects of aripiprazole exposure on monoaminergic and glutamatergic receptor subtypes: comparison with cariprazine. CNS Spectr. 2017 Dec;22(6):484-494. doi: 10.1017/S1092852916000894. Epub 2017 Jan 6. PMID: 28059046.

Aripiprazole/阿立哌唑 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.15mL

2.23mL

1.12mL

22.30mL

4.46mL

2.23mL

Aripiprazole/阿立哌唑 技术信息

CAS号129722-12-9
分子式C23H27Cl2N3O2
分子量 448.39
SMILES Code ClC1=CC=CC(N2CCN(CCCCOC3=CC=C4CCC(=O)NC4=C3)CC2)=C1Cl
MDL No. MFCD00892072
别名 OPC-14597; OPC 31
运输蓝冰
InChI Key CEUORZQYGODEFX-UHFFFAOYSA-N
Pubchem ID 60795
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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