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  • To characterize the human cytochrome P450 forms involved in dimemorfan oxidation (DFO), human liver microsomes, and recombinant P450s were investigated. Liquid chromatography-mass spectral analysis suggested that metabolite (M)1 ([M+H](+) m/z at 272.200) and M2 ([M+H](+) m/z at 242.190) were d-3-hydroxymethyl-N-methylmorphinan and d-3-methylmorphinan, respectively. Kinetic analyses of microsomal DFO showed that the substrate concentration showing a half-maximal velocity (S(50)) of M1 formation was less than that of M2. Microsomal M1 and M2 formation activities correlated significantly with the CYP2D6 marker, dextromethorphan O-demethylation activity. The results indicated the participation of multiple P450 forms in DFO.
  • To characterize the human cytochrome P450 forms involved in dimemorfan oxidation (DFO), human liver microsomes, and recombinant P450s were investigated. Liquid chromatography-mass spectral analysis suggested that metabolite (M)1 ([M+H](+) m/z at 272.200) and M2 ([M+H](+) m/z at 242.190) were d-3-hydroxymethyl-N-methylmorphinan and d-3-methylmorphinan, respectively. Kinetic analyses of microsomal DFO showed that the substrate concentration showing a half-maximal velocity (S(50)) of M1 formation was less than that of M2. Microsomal M1 and M2 formation activities correlated significantly with the CYP2D6 marker, dextromethorphan O-demethylation activity. The results indicated the participation of multiple P450 forms in DFO. (en)
Title
  • The oxidative metabolism of dimemorfan by human cytochrome P450 enzymes
  • The oxidative metabolism of dimemorfan by human cytochrome P450 enzymes (en)
skos:prefLabel
  • The oxidative metabolism of dimemorfan by human cytochrome P450 enzymes
  • The oxidative metabolism of dimemorfan by human cytochrome P450 enzymes (en)
skos:notation
  • RIV/75010330:_____/10:00008753!RIV11-MZ0-75010330
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • V
http://linked.open...iv/cisloPeriodika
  • 2
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  • 277875
http://linked.open...ai/riv/idVysledku
  • RIV/75010330:_____/10:00008753
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  • metabolism; dimemorfan; cytochrome P450 (en)
http://linked.open.../riv/klicoveSlovo
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  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [3AA1C0457006]
http://linked.open...i/riv/nazevZdroje
  • Journal of pharmaceutical sciences
http://linked.open...in/vavai/riv/obor
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http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 99
http://linked.open...iv/tvurceVysledku
  • Souček, Pavel
  • Chau, G.Y.
  • Chi, C. W.
  • Chung, Y. T.
  • Liu, T.Y.
  • Ueng, Y.F.
  • Lee, C. H.
  • Chou, Y.C.
  • Gelboin, H. V.
  • Krausz, K. W.
  • Wang, S. Y.
http://linked.open...ain/vavai/riv/wos
  • 000274114100043
issn
  • 0022-3549
number of pages
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