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KMID : 0043320060290110984
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Archives of Pharmacal Research
2006 Volume.29 No. 11 p.984 ~ p.989
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Identification of 1-Furan-2-yl-3-pyridin-2-yl-propenone, an Anti-inflammatory Agent, and Its Metabolites in Rat Liver Subcellular Fractions
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Lee Sang-Kyu
Jeon Tae-Won
Basnet Arjun
Jeong Hye-Gwang
Lee Eung-Seok
Jeong Tae-Cheon
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Abstract
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1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) has been characterized to have an anti-inflammatory activity through the inhibition of the production of nitric oxide and tumor necrosis . In the present studies, the phase 1 metabolism of FPP-3 was investigated in rat liver microsomes and cytosols. When FPP-3 was incubated with rat liver microsomes and cytosols in the presence of NADPH. 2 major peaks were detected on a liquid chromatography/electrospray ionization-mass spectrometry. Two metabolites (i.e., M1 and M2) were characterized as reduced forms on propenone: M1 (1-furan-2-yl-3-pyridin-2-yl-propan-1-one) was the initial metabolite and M2 (1-furan-2-yl-3-pyridin-2-yl-propan-1-ol) was a secondary alcohol believed to be formed from M1.
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KEYWORD
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1-Furan-2-yl-3-pyridin-2-yl-propenone, LC-ESI/MS, Reduction, Metabolite
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