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Iloperidone

Iloperidone

产品编号 T1539   CAS 133454-47-4
别名: 伊潘立酮, HP 873

Iloperidone 是一种D2/5-HT2受体拮抗剂,是非典型抗精神病药,可治疗精神分裂症。

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Iloperidone, CAS 133454-47-4
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产品目录号及名称: Iloperidone (T1539)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Iloperidone is an atypical antipsychotic agent that is used for treatment of schizophrenia.
靶点活性 dopamine D3 receptor:7.1 nM(ki), dopamine D4 receptor:25 nM(ki)
体外活性 Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors. [1] Iloperidone displays higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 nM and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). [2] Iloperidone significantly increases dopa accumulation, an index of dopamine turnover in response to D2 receptor blockade, at doses from 0.3 mg/kg to 10 mg/kg i.p. in the striatum and from 1 mg/kg to 10 mg/kg in the nucleus accumbens. [3]
体内活性 Iloperidone exerts behavioral effects in pharmacological rats models of disrupted sensorimotor gating consistent with "atypical" antipsychotics, mediated by antagonism of dopaminergic and noradrenergic receptors. Iloperidone (1 and 3 mg/kg) prevents the PPI-disruptive effects of treatment with 1 mg/kg PCP. Iloperidone (0.3 mg/kg) prevents cirazoline-induced PPI deficits, independent of its effects on startle magnitude. [4] Iloperidone (10 mg/kg) and Melperone (10 mg/kg) produce an equivalent or a smaller increase in DA release in the nucleus accumbens (NAC) of rats, respectively, compared to the mPFC, whereas none of them increase acetylcholine (ACh) release in the NAC. [5]
激酶实验 Immunoblotting for the mTOR kinase assay: HEK293 cells are plated at 2-2.5&times;105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr
别名 伊潘立酮, HP 873
分子量 426.4806
分子式 C24H27FN2O4
CAS No. 133454-47-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: 4 mg/mL (9.37 mM)

H2O: <1 mg/mL

DMSO: 26 mg/mL (61 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Kalkman HO, et al. Neuropsychopharmacology, 2001, 25(6), 904-914. 2. Kongsamut S, et al. Eur J Pharmacol, 1996, 317(2-3), 417-423. 3. Szczepanik AM, et al. J Pharmacol Exp Ther, 1996, 278(2), 913-920. 4. Barr AM, et al. Neuropharmacology, 2006, 51(3), 457-465. 5. Ichikawa J, et al. Brain Res, 2002, 956(2), 349-357. 6. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy[J]. Toxicology and Applied Pharmacology. 2020, 406: 115239.

文献引用

1. Danek P J, Kuban W, Daniel W A. The Effect of Chronic Iloperidone Treatment on Cytochrome P450 Expression and Activity in the Rat Liver: Involvement of Neuroendocrine Mechanisms. International Journal of Molecular Sciences. 2021, 22(16): 8447. 2. Qian H Y, Zhou F, Wu R, et al. Metformin Attenuates Bone Cancer Pain by Reducing TRPV1 and ASIC3 Expression. Frontiers in Pharmacology. 2021: 1924. 3. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy. Toxicology and Applied Pharmacology. 2020, 406: 115239
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相关化合物库

该产品包含在如下化合物库中:
上市药物库 儿童药物库 抗癌上市药物库 ReFRAME 相关化合物库 抗心血管疾病化合物库 神经递质受体化合物库 抗COVID-19化合物库 抗癌化合物库 NO PAINS 化合物库 含氟化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Iloperidone 133454-47-4 GPCR/G Protein Neuroscience 5-HT Receptor Dopamine Receptor Adrenergic Receptor 伊潘立酮 Inhibitor 5-hydroxytryptamine Receptor atypical Serotonin Receptor inhibit symptoms HP873 HP-873 antipsychotic schizophrenia HP 873 inhibitor

 

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