Activation of mianserin and its metabolites by human liver microsomes.

@article{Lambert1989ActivationOM,
  title={Activation of mianserin and its metabolites by human liver microsomes.},
  author={C. Lambert and B. K. Park and N. Kitteringham},
  journal={Biochemical pharmacology},
  year={1989},
  volume={38 17},
  pages={
          2853-8
        }
}
Human liver microsomes metabolise mianserin to the stable 8-hydroxymianserin, desmethylmianserin and mianserin-2-oxide and in addition to one or more chemically reactive metabolites which bind, irreversibly, to microsomal protein. The stable metabolites were isolated by HPLC and characterized by mass spectrometry. The generation of each of these metabolites showed substantial inter-individual variation between eight sets of human liver microsomes studied. Inhibition of irreversible binding was… Expand
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Analysis of stable metabolites revealed that mianserin is activated to a cytotoxic metabolite selectively by a constitutive form of human cytochrome P-450, whereas phenytoin, amitriptyline and imipramine are selectively activated by forms of mouse cyto Chrome which are induced by either phenobarbitone or beta-naphthoflavone. Expand
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