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别名 | OPC-14597 | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C23H27Cl2N3O2 |
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分子量 | 448.39 | CAS号 | 129722-12-9 | |
Solubility (25°C)* | 体外 | DMSO | 90 mg/mL (200.71 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist. | ||
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体外研究 | Aripiprazole以高亲和力结合与G蛋白耦合和未耦合状态的受体。Aripiprazole有效激活D2受体介导的对cAMP积聚的抑制。[1] Aripiprazole对h5-HT(2B)-,hD(2L)-,和hD(3)-多巴胺受体具有最高亲和力,但是也对几种其他5-HT受体(5-HT(1A),5-HT(2A),5-HT(7)),以及α(1A)-肾上腺素能和hH(1)-组氨酸受体具有显著亲和力(5-30 nM)。Aripiprazole对其他G蛋白耦合的受体,包括5-HT(1D),5-HT(2C),α(1B)-,α(2A)-,α(2B)-,α(2C)-,β (1)-,和β(2)-肾上腺素能,以及H(3)-组氨酸受体具有较低亲和力(30-200 nM)。Aripiprazole是一种5-HT(2B)受体的反向激动剂,并对5-HT(2A),5-HT(2C),D(3),和D(4)表现出部分激动作用。[2] | ||
体内研究 | Aripiprazole降低未用药大鼠内侧前额叶皮质和纹状体中细胞外5-HIAA浓度, 但是对长期Aripiprazole预处理的大鼠没有影响。[3] Aripiprazole,0.1 mg/kg和0.3 mg/kg,显著增加大鼠海马体中多巴胺的释放。Aripiprazole,0.3 mg/kg,略微但显著增加内侧前额叶皮质中多巴胺的释放,但不影响伏隔核中多巴胺的释放。Aripiprazole,3.0 mg/kg和10 mg/kg,显著减少伏隔核中多巴胺的释放,但对内侧前额叶皮质没有影响。Aripiprazole,0.3 mg/kg,瞬时增强haloperidol (0.1 mg/kg)诱导的内侧前额叶皮质中多巴胺释放,但在伏隔核中产生抑制作用。[4] |
数据来源于[Data independently produced by , , J Psychiatr Res, 2017, 88:18-27 ]
数据来源于[Data independently produced by , , J Psychiatr Res, 2018, 105:95-102]
Chronic Aripiprazole and Trazodone Polypharmacy Effects on Systemic and Brain Cholesterol Biosynthesis [ Biomolecules, 2023, 10.3390/biom13091321] | PubMed: 37759721 |
Chronic Aripiprazole and Trazodone Polypharmacy Effects on Systemic and Brain Cholesterol Biosynthesis [ Biomolecules, 2023, 13(9)1321] | PubMed: 37759721 |
Individual and simultaneous treatment with antipsychotic aripiprazole and antidepressant trazodone inhibit sterol biosynthesis in the adult brain [ J Lipid Res, 2022, 63(8):100249] | PubMed: 35839864 |
JAK2 Inhibitor, Fedratinib, Inhibits P-gp Activity and Co-Treatment Induces Cytotoxicity in Antimitotic Drug-Treated P-gp Overexpressing Resistant KBV20C Cancer Cells [ Int J Mol Sci, 2022, 23(9)4597] | PubMed: 35562984 |
Terconazole, an Azole Antifungal Drug, Increases Cytotoxicity in Antimitotic Drug-Treated Resistant Cancer Cells with Substrate-Specific P-gp Inhibitory Activity [ Int J Mol Sci, 2022, 23(22)13809] | PubMed: 36430288 |
Effects of Psychotropic Medication on Somatic Sterol Biosynthesis of Adult Mice [ Biomolecules, 2022, 12(10)1535] | PubMed: 36291744 |
Social-like responses are inducible in asocial Mexican cavefish despite the exhibition of strong repetitive behavior [ Elife, 2021, 10e72463] | PubMed: 34542411 |
Inhibition of Arenaviruses by Combinations of Orally Available Approved Drugs [ Antimicrob Agents Chemother, 2021, AAC.01146-20] | PubMed: 33468464 |
Cox15 is a novel oncogene that required for lung cancer cell proliferation [ Biochem Biophys Res Commun, 2021, 578:70-76] | PubMed: 34547626 |
Second generation atypical antipsychotics olanzapine and aripiprazole reduce expression and secretion of inflammatory cytokines in human immune cells [Stapel B J Psychiatr Res, 2018, 105:95-102] | PubMed: 30216787 |
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