Metabolic Studies of Aminopyrine in Rat and Man by Using Stable Isotope Tracer Techniques

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The metabolites of aminopyrine (AM) were analyzed by using stable isotope tracer techniques. After the oral administration of an equimolar mixture of AM and AM-2-CD_3 (mixture 1), or an equimolar mixture of AM-3-CH_2OH and AM-3-CD_2OH (mixture 2), or either AM-3-CD_3 or AM-4-N (CD_3)_2 to rats, the urinary metabolites were extracted with chloroform at pH 7.0,and the extracts were subjected to gas chromatography-mass spectrometry after trimethylsilylation. Characteristic doublet peaks in the mass spectra indicated the presence of a metabolite originating from mixture 1 or 2 mentioned above. The new metabolites detected by gas chromatography-mass spectrometry (GC-MS) were identified as 3-hydroxymethyl-4-monomethylaminoantipyrine (MAA-3-CH_2OH) and 3-hydroxymethyl-4-aminoantipyrine (AA-3-CH_2OH) from the shifts of the mass numbers of the molecular ions after the administration of AM-3-CD_3 and AM-4-N(CD_3)_2. Two other metabolites were newly detected following the administration of mixture 2(AM-3-CH_2OH is an intermediary metabolite of AM) to rats. They were identified as 3-hydroxymethyl-4-acetylaminoantipyrine (AcMAA-3-CH_2OH) and 3-hydroxymethyl-4-acetylaminoantipyrine (AcAA-3-CH_2OH). MAA-3-CH_2OH was also detected in human urine after the oral administration of AM.
社団法人日本薬学会の論文
1981-06-25