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.
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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。 |
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]. |
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 << |
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 |
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
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