Quetiapine

(Synonyms: 喹硫平; ICI204636)
目录号: PL09255 纯度: ≥99%
Quetiapine (ICI204636) 是一种 5-HT 受体激动剂,对人 5-HT1A 的 pEC50 值为 4.77。Quetiapine 是多巴胺受体 (dopamine receptor) 拮抗剂,对人 D2 的 pIC50 值为 6.33。Quetiapine 对人 D2,HT1A,5-HT2A,5-HT2C 受体具有中高等亲和力,pKi 值为 7.25,5.74,7.54,5.55。具有抗抑郁和抗焦虑作用。
CAS No. :111974-69-7
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中文名称
Quetiapine
中文别名
喹硫平;11-[4-[2-(2-羟基乙氧基)乙基]-1-哌嗪基]二苯并[b,f][1,4]硫氮杂卓;庚酸乙酯;喹硫平富马酸盐;喹硫平杂质;富马酸喹硫平D4
英文名称
Quetiapine
英文别名
QUETIAPINE-D4 FUMARATE;QUETIAPIN;2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]-ethanol;Quetiapine;11-[4-[2-(2-Hydroxyethoxy)ethyl]piperazino]dibenzo[b,f][1,4]thiazepine;2-[2-[4-[Dibenzo[b,f][1,4]thiazepin-11-yl]piperazin-1-yl]ethoxy]ethanol;2-(2-(4-(Dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)ethoxy)ethanol;2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol;[14C]-Quetiapine;11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine;2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol;Co-Quetiapine;quetiapina;Quetiapine [INN:BAN];quetiapinum;Seroquel;UNII-BGL0JSY5SI;uetiapine;Ketipinor;Dibenzo[b,f][1,4]thiazepine, ethanol deriv.;2-[2-(4-benzo[b][1,5]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol
Cas No.
111974-69-7
分子式
C21H25N3O2S
分子量
383.51
包装储存
Pure form -20°C 3 years;4°C 2 years
产品详情
Quetiapine (ICI204636) 是一种 5-HT 受体激动剂,对人 5-HT1A 的 pEC50 值为 4.77。Quetiapine 是多巴胺受体 (dopamine receptor) 拮抗剂,对人 D2 的 pIC50 值为 6.33。Quetiapine 对人 D2,HT1A,5-HT2A,5-HT2C 受体具有中高等亲和力,pKi 值为 7.25,5.74,7.54,5.55。具有抗抑郁和抗焦虑作用。
生物活性
Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC 50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC 50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK i s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
性状
Oil
IC50 & Target[1][2]
5-HT1A Receptor 5.74 (pKi) 5-HT2A Receptor
体外研究(In Vitro)
Quetiapine (<100?μM; 24?hours) has no significant effect on cell viabilities.
Quetiapine (10?μM) inhibits NO release, which increased by LPS (0.1-100 ng/mL) in concentration-dependent manner.
Quetiapine (10?μM) also inhibits TNF-α synthesis.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
Quetiapine (10?mg/kg/day; ingested) can alleviate the recruitment and activation of microglia and promote myelin repair in Cuprizone (CPZ)-induced chronic mouse model of demyelination. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Cross AJ, et al. Quetiapine and its metabolite norquetiapine: translation from in vitro pharmacology to in vivo efficacy in rodent models. Br J Pharmacol. 2016 Jan;173(1):155-66.
[2]. Hanzhi Wang, et al. Quetiapine Inhibits Microglial Activation by Neutralizing Abnormal STIM1-Mediated Intercellular Calcium Homeostasis and Promotes Myelin Repair in a Cuprizone-Induced Mouse Model of Demyelination. Front Cell Neurosci. 2015 Dec 21;9:492.
溶解度数据
In Vitro: Ethanol : 100 mg/mL (260.75 mM; Need ultrasonic)DMSO : 100 mg/mL (260.75 mM; Need ultrasonic)H2O : 0.1 mg/mL (0.26 mM; ultrasonic and warming and heat to 50°C)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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