Analytical studies on mepirizole and its metabolites. II. Identification of the human urinary metabolites of mepirizole with stable isotope labeling.

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Abstract
The metabolism of [the analgesic, anti inflammation drug] mepirizole (I) in human urine was studied by labeling the drug with a stable isotope, deuterium. An equimolar mixture of the 2H-1 labeled mepirizole (II) and its protium counterpart (I) was administered orally to a man. The metabolites were extracted from the pooled urine with CH2CL2, treated with diazomethane and applied to GC-MS [gas chromatography-1 mass spectroscopy]. The ion clusters in the mass spectra were used for detection of the urinary metabolites of I in man. By this technique, 3 metabolites, 1-(4-methoxy-6-methyl-2-pyrimidinyl)-5-methoxy-3-hydroxymethylpyrazole, 1-(4-methoxy-6-methyl-2-pyrimidinyl)-5-methoxypyrazole-3-carboxylic acid and 1-(4-methoxy-6-carboxy-2-pyrimidinyl)-5-methoxy-3-methylpyrazole were identified in human urine.

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