In vitro metabolism of a novel phosphodiesterase-5 inhibitor DA-8159 in rat liver preparations using liquid chromatography/electrospray mass spectrometry.
作者： Sung Jin Choi , Hye Young Ji , Hee-Yong Lee , Dong Sung Kim , Won Bae Kim
DOI: 10.1002/BMC.173
关键词:
摘要: The in vitro metabolism of a new erectogenic, DA-8159, has been studied by LC with UV detection and on-line LC-electrospray mass spectrometry using rat hepatic microsomal incubation liver perfusion. Both DA-8159 the presence NADPH single-pass perfusion resulted formation three metabolites (M1–3). M1 was tentatively identified as hydroxy-DA-8159. M2 M3 were N-demethyl-DA-8159 5-(2-propyloxy-5-aminosulphonylphenyl)-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidin-7-one (DA-8164), respectively, on basis LC-MS/MS analysis authentic standards. Rat CYP2D1 major isozyme for hydroxy-DA-8159 N-demethyl-DA-8159. CYP2C12 CYP1A1 catalysed oxidation to DA-8164. Copyright © 2002 John Wiley & Sons, Ltd.
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