1. Immunology/Inflammation
    Metabolic Enzyme/Protease
  2. COX
    Drug Metabolite
  3. 4-Methylamino antipyrine

4-Methylamino antipyrine 

Cat. No.: HY-135731
Handling Instructions

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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4-Methylamino antipyrine Chemical Structure

4-Methylamino antipyrine Chemical Structure

CAS No. : 519-98-2

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Description

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[1][2][3]. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties[2].

IC50 & Target
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[2].

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[1].

Molecular Weight

217.27

Formula

C₁₂H₁₅N₃O

CAS No.

519-98-2

SMILES

O=C1N(C2=CC=CC=C2)N(C)C(C)=C1NC

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

4-Methylamino antipyrineCOXDrug MetaboliteCyclooxygenaseNSAIDMetamizolemetabolitenonopioidanalgesicantipyretic anti-inflammatoryInhibitorinhibitorinhibit

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4-Methylamino antipyrine
Cat. No.:
HY-135731
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