Oxidation of 5-methoxy-N,N-diisopropyltryptamine in rat liver microsomes and recombinant cytochrome P450 enzymes
作者： Shizuo Narimatsu , Rei Yonemoto , Kazufumi Masuda , Takashi Katsu , Masato Asanuma
DOI: 10.1016/J.BCP.2007.09.019
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摘要: Abstract The oxidative metabolism of 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT), a tryptamine-type designer drug, was studied using rat liver microsomal fractions and recombinant cytochrome P450 (CYP) enzymes. 5-MeO-DIPT biotransformed mainly into side-chain N-deisopropylated metabolite partially an aromatic ring O-demethylated in from untreated rats both sexes. This metabolic profile is different our previous findings human fractions, which the O-demethylation major pathway whereas N-deisopropylation minor [Narimatsu S, Yonemoto R, Saito K, Takaya Kumamoto T, Ishikawa et al. Oxidative (Foxy) by microsomes Biochem Pharmacol 2006;71:1377–85]. Kinetic inhibition studies indicated that N-dealkylation mediated CYP2C11 CYP3A2, CYP2D2 CYP2C6 male rats. Pretreatment with β-naphthoflavone (BNF) produced 6-hydroxylated metabolite. Recombinant CYP1A1 efficiently catalyzed 6-hydroxylation under conditions used. These results provide valuable information on fate can be used toxicological study this drug.
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