4-(甲氨基)安替比林

中文名称:

4-(甲氨基)安替比林

中文同义词:

4-(甲基氨基)安替比林;咪达唑仑杂质C;2,3-二甲基-4-甲基-1-苯基-3-吡唑啉-5-酮;1,2-二氢-1,5-二甲基-4-(甲基氨基)-2-苯基-3H-吡唑-3-酮;4-(甲氨基)安替比林;安替比林,4-(甲基氨基)-;乙二醇甲酸乙醚1,5-二甲基-4-(甲基氨基)-2-苯基-;4-单甲基氨基安替比林

英文名称:

1,2-dihydro-1,5-dimethyl-4-(methylamino)-2-phenyl-3H-pyrazol-3-one

英文同义词:

2-(1-cyclohexa-2,4-dienyl)-1,5-dimethyl-4-(methylamino)-3-pyrazolone;noramidopyrine;4-(Methylamino)-antipyrine;2,3-Dimethyl-4-methylamino-1-phenyl-3-pyrazolin-5-one;Methylaminoantipyrine;Monomethylaminoantipyrine;Noraminopyrine;1,5-Dimethyl-4-(methylamino)-2-phenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride

CAS号:

519-98-2

分子式:

C12H15N3O

分子量:

217.27

EINECS号:

208-281-3

相关类别:

对照品-杂质对照品;其他兽药标准品;中药对照品;标准品;药物杂质及中间体;Aromatics;Heterocycles;Intermediates Fine Chemicals;Metabolites Impurities;Pharmaceuticals

Mol文件:

519-98-2.mol

熔点 

50-53°C

沸点 

324.5±45.0 °C(Predicted)

密度 

1.20±0.1 g/cm3 (20 ºC 760 Torr)

储存条件 

-20°C Freezer

酸度系数(pKa)

4.76±0.20(Predicted)

生物活性

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 是一种非阿片类镇痛药，可用于疼痛和发烧。4-Methylamino antipyrine 具有止痛，解热和相对较弱的抗炎特性。

靶点

COX

体外研究

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.

体内研究

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.

化学性质 

油状液体。

用途 

安乃近的中间体。

生产方法 

用氨基安替比林以甲酸甲酰化，生成4-（甲酰氨基）安替比林，然后以硫酸二甲酯在碱性条件下甲基化，得4-甲酰甲氨基安替比林，将后者以硫酸水解（去除甲酰基）并中和制得该品。

HazardClass 

IRRITANT

毒性

LD50 oral in mouse: 7gm/kg