Staack, R. F.; Theobald, D. S.; Paul, L. D.; Springer, D.; Kraemer, T.; Maurer, H. H. published the article 《In vivo metabolism of the new designer drug 1-(4-methoxyphenyl)piperazine (MeOPP) in rat and identification of the human cytochrome P450 enzymes responsible for the major metabolic step》. Keywords: methoxyphenylpiperazine metabolism cytochrome P450 2D6.They researched the compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8 ).Recommanded Product: 56621-48-8. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:56621-48-8) here.
The in vivo metabolism of 1-(4-methoxyphenyl)piperazine (MeOPP), a novel designer drug, was studied in male Wistar rats. MeOPP was mainly O-demethylated to 1-(4-hydroxyphenyl)piperazine (4-HO-PP) in addition to degradation of the piperazine moiety. O-demethylation, the major metabolic step, was studied with cDNA-expressed human hepatic cytochrome P 450 (CYP) enzymes in pooled human liver microsomes (pHLM) and in single donor human liver microsomes with CYP2D6 poor metabolizer genotype (PM HLM). CYP2D6 catalyzed O-demethylation with apparent Km and Vmax values of 48.34 μM and 5.44 pmol min-1 pmol-1 CYP, resp. pHLM catalyzed the monitored reaction with an apparent Km = 204.80 μM and Vmax = 127.50 pmol min-1 mg-1 protein. The CYP2D6-specific chem. inhibitor quinidine (1 and 3 μM) significantly inhibited 4-HO-PP formation by 71.9% and by 98.5%, resp., in incubation mixtures with pHLM and 200 μM MeOPP. O-demethylation was significantly lower in PM HLM compared with pHLM (70.6%). These data suggest that polymorphically expressed CYP2D6 is the enzyme mainly responsible for MeOPP O-demethylation.
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