4-Methylamino antipyrine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

4-Mmethylamino antipyrine 是安乃近的活性代谢物。安乃近是一种吡唑啉酮类非甾体抗炎化合物 (NSAID)，可抑制 COX。

4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak anti-inflammatory properties.(In Vitro):At room temperature and in an atmosphere with oxygen, Metamizole 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 .(In Vivo):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 concentration of 4-Methylamino antipyrine is 47.59 mg/mL. The average half-lives is 8.57 h for 4-Methylamino antipyrine .

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.

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.

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Chromatin/Epigenetic

COX

CRAC channel

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519-98-2

217.272

C12H15N3O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (230.13 mM)

CNc1c(C)n(C)n(-c2ccccc2)c1=O

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(-20℃)

With Ice Pack

≥ 2 years