Aripiprazole

製品コードS1975 バッチS197503

印刷

化学情報

Chemical Structure Synonyms OPC-14597 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H27Cl2N3O2
分子量 448.39 CAS No. 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
in vitro Aripiprazole binds with high affinity to both the G protein-coupled and uncoupled states of receptors. Aripiprazole potently activates D2 receptor-mediated inhibition of cAMP accumulation. [1] Aripiprazole has highest affinity for h5-HT(2B)-, hD(2L)-, and hD(3)-dopamine receptors, but also has significant affinity (5-30 nM) for several other 5-HT receptors (5-HT(1A), 5-HT(2A), 5-HT(7)), as well as alpha(1A)-adrenergic and hH(1)-histamine receptors. Aripiprazole has less affinity (30-200 nM) for other G protein-coupled receptors, including the 5-HT(1D), 5-HT(2C), alpha(1B)-, alpha(2A)-, alpha(2B)-, alpha(2C)-, beta(1)-, and beta(2)-adrenergic, and H(3)-histamine receptors. Aripiprazole is an inverse agonist at 5-HT(2B) receptors and displays partial agonist actions at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors. [2]
in vivo Aripiprazole reduces extracellular 5-HIAA concentrations in the medial prefrontal cortex and striatum of drug-naive rats, but not in chronic Aripiprazole-pretreated rats. [3] Aripiprazole, 0.1 mg/kg and 0.3 mg/kg, significantly increases dopamine release in the hippocampus of rats. Aripiprazole, 0.3 mg/kg, slightly but significantly increases dopamine release in the medial prefrontal cortex but not in the nucleus accumbens. Aripiprazole, 3.0 mg/kg and 10 mg/kg, significantly decreases dopamine release in the nucleus accumbens but not the medical prefrontal cortex. Aripiprazole, 0.3 mg/kg, transiently potentiates haloperidol (0.1 mg/kg)-induced dopamine release in the medial prefrontal cortex but inhibited that in the nucleus accumbens. [4]

プロトコル(参考用のみ)

カスタマーフィードバック

Data from [Data independently produced by , , J Psychiatr Res, 2017, 88:18-27 ]

Data from [Data independently produced by , , J Psychiatr Res, 2018, 105:95-102]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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