Quetiapine
(Synonyms: 喹硫平; ICI204636) 目录号 : GC14167
Quetiapine是一种5-HT受体激动剂，对人类5-HT1A受体的 pEC50为4.77。Quetiapine是一种多巴胺受体拮抗剂，对人类D2受体的pIC50为6.33。Quetiapine是一种非典型抗精神病药，用于治疗精神分裂症、躁郁症和重度抑郁症。
Cas No.:111974-69-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | Human skin keratinocytes cell |
Preparation Method | Human skin keratinocytes, HaCaT, were cultured in DMEM supplemented with 10% heat-inactivated fetal bovine serum at 37°C in 5% CO2. The cells were incubated with or without Quetiapine for 12h prior to UVB irradiation. Then, the cells were washed with phosphate buffered saline (PBS; pH7.4) and irradiated using a UVB lamps. The irradiation intensity was monitored by a UVB radiometer. Immediately after UVB irradiation, the cells were returned to the incubator and incubated with drug-free medium for 24h. |
Reaction Conditions | 10, 20, 50μg/mL; 12h |
Applications | The Quetiapine-treated group had significantly lower levels of MDA and significantly higher activities of SOD and GSH-Px compared to the UVB and PBS groups. |
| Animal experiment [2]: | |
Animal models | UVB Irradiation Model |
Preparation Method | Quetiapine was dissolved in Dimethyl sulfoxide (DMSO) and diluted in phosphate-buffered salt solution (PBS). the working concentration of Quetiapine was the minimum maintenance dose (400mg/mL) used in clinics.Mice were randomly divided into 4 groups that represented treatments or controls. These were: normal healthy controls (no UVB or treatment), UVB irradiation alone (no treatment), UVB irradiation following a sham phosphate buffered saline (PBS) treatment (PBS group), and UVB following Quetiapine treatment (Quetiapine group). Each of these 4 groups was sub-divided randomly into 4 subgroups, which represented various time points to be investigated. Before experimentation, mice were anesthetized by intraperitoneal injection of 1% sodium pentobarbital and hair was removed from the back skin of mice using hair removal wax. Mice were placed 10cm below the lamps, the back skin of mice was collected at 0, 6, 12 and 24h. |
Dosage form | 400mg/mL; surface application; 0, 6, 12 and 24h |
Applications | Quetiapine treatment was able to significantly decrease skin thickness, erythema, and edema, as well as inflammation. Quetiapine treatment increased the activities of antioxidant enzymes, including superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). In addition, it reduced the production of malondialdehyde (MDA), a kind of oxidized lipid. |
References: | |
Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine is an atypical antipsychotic used to treat schizophrenia, bipolar disorder, and major depressive disorder[1].
Quetiapine (1, 10μM; 48h) causes cell cycle exit and promotes cell differentiation in primary oligodendrocyte cultures[2].Quetiapine (10, 20, 50μg/mL; 12h) treated had significantly lower levels of MDA and significantly higher activities of SOD and GSH-Px[3].Quetiapine (<100μM; 24h) has no significant effect on cell viabilities[4].
Quetiapine (400 mg/mL; surface application; 0, 6, 12, 24h) treatment significantly reduced skin thickening, erythema and edema, and inflammation caused by UVB irritation. In addition, Quetiapine treatment increased the activity of antioxidant enzymes, including superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), while reducing the production of the oxidised lipid malondialdehyde (MDA)[3].Quetiapine (10, 30, 100mg/kg; po; bid; 28d) elicited a statistically significant, dose-dependent decrease in METH-induced hyperlocomotion 0.5h after administration. There were Quetiapine-induced, dose-dependent decreases in locomotor activity at 8 and 12h[4].
References:
[1].Cross A J, Widzowski D, Maciag C, et al. Quetiapine and its metabolite norQuetiapine: translation from in vitro pharmacology to in vivo efficacy in rodent models[J]. British journal of pharmacology, 2016, 173(1): 155-166.
[2].Mi G, Wang Y, Ye E, et al. The antipsychotic drug Quetiapine stimulates oligodendrocyte differentiation by modulating the cell cycle[J]. Neurochemistry International, 2018, 118: 242-251.
[3]. Xu P, Zhang M, Wang X, et al. Antioxidative effect of Quetiapine on acute ultraviolet-B-induced skin and HaCaT cell damage[J]. International Journal of Molecular Sciences, 2018, 19(4): 953.
[4] Kondo M A, Tajinda K, Colantuoni C, et al. Unique pharmacological actions of atypical neuroleptic Quetiapine: possible role in cell cycle/fate control[J]. Translational psychiatry, 2013, 3(4): e243-e243.
Quetiapine是一种5-HT受体激动剂，对人类5-HT1A受体的pEC50为4.77。Quetiapine是一种多巴胺受体拮抗剂，对人类D2受体的 pIC50为6.33。Quetiapine是一种非典型抗精神病药，用于治疗精神分裂症、躁郁症和重度抑郁症[1]。
Quetiapine（1，10μM；48h）导致细胞周期退出并促进原代少突胶质细胞培养中的细胞分化[2]。Quetiapine（10，20，50μg/mL；12h）处理的MDA水平显著降低，SOD和GSH-Px活性显著升高[3]。Quetiapine（<100μM；24h）对细胞活力没有显著影响[4]。
Quetiapine（400mg/mL；surface application；0、6、12、24h）治疗能够显著减少UVB刺激引起的皮肤增厚、红斑和水肿以及炎症。此外，Quetiapine治疗可增加抗氧化酶的活性，包括超氧化物歧化酶 (SOD)和谷胱甘肽过氧化物酶(GSH-Px)，同时减少了氧化脂质丙二醛 (MDA) 的产生[3]。Quetiapine（10、30、100mg/kg；po；bid；28d）在给药后0.5小时引起METH诱导的过度运动出现统计学上显著的剂量依赖性下降。在8小时和12小时，Quetiapine诱导的运动活性出现剂量依赖性下降[4]。
| Cas No. | 111974-69-7 | SDF | |
| 别名 | 喹硫平; ICI204636 | ||
| 化学名 | 2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol | ||
| Canonical SMILES | C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42 | ||
| 分子式 | C21H25N3O2S | 分子量 | 383.51 |
| 溶解度 | 100mg/mL in DMSO（ultrasonic and warming and heat to 45°C), ≥ 29.55 mg/mL in EtOH with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6075 mL | 13.0375 mL | 26.0749 mL |
| 5 mM | 0.5215 mL | 2.6075 mL | 5.215 mL |
| 10 mM | 0.2607 mL | 1.3037 mL | 2.6075 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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