4-(甲氨基)安替比林

生物活性靶点体外研究体内研究 4-(甲氨基)安替比林试剂级价格

4-(甲氨基)安替比林

CAS号:519-98-2
英文名:1,2-dihydro-1,5-dimethyl-4-(methylamino)-2-phenyl-3H-pyrazol-3-one
中文名:4-(甲氨基)安替比林
CBNumber:CB5924116
分子式:C12H15N3O
分子量:217.27
MOL File:519-98-2.mol

4-(甲氨基)安替比林化学性质

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
溶解度 :Chloroform (Slightly), Ethyl Acetate (Slightly), Methanol (Slightly)
形态 :Solid
酸度系数(pKa) :4.76±0.20(Predicted)
颜色 :Pale Yellow to Brown

安全信息

危险等级 :IRRITANT
毒性 :LD50 oral in mouse: 7gm/kg

4-(甲氨基)安替比林性质、用途与生产工艺

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。