Aripiprazole

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Chemical Structure| 129722-12-9 同义名 : OPC-14597; OPC 31
CAS号 : 129722-12-9
货号 : A134405
分子式 : C23H27Cl2N3O2
纯度 : 98%
分子量 : 448.39
MDL号 : MFCD00892072
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
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 <<
实验方案
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

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.