Metabolism of FPP-3, an Anti-inflammatory Propenone Compound, in Rat by Liquid Chromatography-Electrospray Ionization Tandem Mass Spectrometry(Biopharmacy)

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1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) is an anti-inflammatory agent with a propenone moiety. Following a single intravenous injection of male Sprague-Dawley rats with 4 mg/kg of FPP-3, three different metabolites of FPP-3 were identified as M1 (1-furan-2-yl-3-pyridin-2-yl-propan-1-one), M2 (1-furan-2-yl-3-pyridin-2-yl-propan-1-ol) and M3 (a glucuronide conjugate of M2) in rat urine by a liquid chromatography-electrospray tandem mass spectrometry. The structures of M1 and M2 were the same as observed previously following the incubation of rat liver microsomes with FPP-3 in the presence of NADPH. Although all metabolites of FPP-3 were identified in rat urine, only M1 and M2 were observed in the bile and feces. In addition, FPP-3 and its metabolites were mostly excreted into the urine. The M3 was identified as a glucuronide conjugate of M2 because of the addition of 176 Da from the protonated molecular ion of M2 in MS^2 and because of the production of free M2 following an incubation of urine with β-glucuronidase. From these studies, a possible metabolic fate of FPP-3 could be proposed in vivo.
公益社団法人日本薬学会の論文
2007-05-01