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| 中文名称 |
4-Methylamino antipyrine
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|---|---|
| 中文别名 |
4-甲基氨基安替比林;4-甲氨基安替比林;1,2-二氢-1,5-二甲基-4-(甲基氨基)-2-苯基-3H-吡唑-3-酮;4-(N-甲基)-氨基安替比林;4-(甲氨基)安替比林;4-(甲基氨基)安替比林;2,3-二甲基-4-甲基-1-苯基-3-吡唑啉-5-酮
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| 英文名称 |
4-Methylamino antipyrine
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| 英文别名 |
1,5-Dimethyl-4-(methylamino)-2-phenyl-1,2-dihydro-3H-pyrazol-3-one;4-Methylamino Antipyrine;1,5-Dimethyl-4-(methylamino)-2-phenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride;3H-Pyrazol-3-one,1,2-dihydro-1,5-dimethyl-4-(methylamino)-2-phenyl-;4 Methylaminoantipyrine;4-Methylamino Antipy;1-phenyl-2,3-dimethyl-4-(N-methylamino)pyrazol-5-one;1-phenyl-2,3-dimethyl-4-methylamino-5-pyrazolone;4-(N-methyl)-aminoantipyrine;4-methylamino-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one;4-methylaminophenazone;4-Monomethylaminoantipyrine;4-Monomethylaminophenazone;ANTIPYRINE,4-(METHYLAMINO);Methylaminoantipyrine;Methylaminophenazone;Monomethylaminoantipyrine;N-Methylaminophenazone;Noramidopyrine;Noramin;Antipyrine,4-(methylamino)- (6CI,8CI);4-(Methylamino)antipyrine;N-Methyl-4-aminoantipyrine;N-Methyl-4-aminophenazone;N-Methylaminoantipyrine;Noraminopyrine;[
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| Cas No. |
519-98-2
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| 分子式 |
C12H15N3O
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| 分子量 |
217.27
|
| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
4-Methylamino antipyrine 是一种 Metamizole 的活性代谢产物。Metamizole 是吡唑啉酮类非甾体抗炎药 (NSAID)，可抑制 COX。Metamizole 是一种非阿片类化合物，可用于疼痛和发烧的研究。
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| 生物活性 |
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
COX
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| 体外研究(In Vitro) |
Metamizole is a prodrug which, at room temperature and in an atmosphere with oxygen, is spontaneously, nonenzymatically converted to 4-Methylamino antipyrine. Subsequently, the N-methyl side chain of 4-Methylamino antipyrine is oxidized to yield 4-formylaminoantipyrine, which is further converted to 4-aminoantipyrine. Metamizole in aqueous solution and in the presence of oxygen consists of a group of several pyrazolone derivatives of which 4-Methylamino antipyrine is pharmacologically the most important. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
The aim of this study is to assess the pharmacokinetics of its active metabolites 4-Methylamino antipyrine in male piglets after a single intramuscular injection of Metamizole. Eight healthy male piglets are administered Metamizole (100 mg/kg) intramuscularly. 4-Methylamino antipyrine plasma concentrations are quantitatively detectable from 0.25 to 48 h. The average maximum concentrations of 4-Methylamino antipyrine is of 47.59 mg/mL. The average half-lives is 8.57 h for 4-Methylamino antipyrine. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| 参考文献 |
[1]. Burmańczuk A, et al. Pharmacokinetic investigations of the marker active metabolites 4-methylamino-antipyrine and 4-amino-antipyrine after intramuscular injection of metamizole in healthy piglets. J Vet Pharmacol Ther. 2016 Dec;39(6):616-620.[2]. Campos C1, et al. Regulation of cyclooxygenase activity by metamizol. Eur J Pharmacol. 1999 Aug 13;378(3):339-47.
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| 溶解度数据 |
In Vitro: DMSO : 50 mg/mL (230.13 mM; Need ultrasonic)配制储备液
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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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