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The in vivo metabolism of 3-oxo-5-benzylidene-6-methyl-(4H)-2-(benzoylmethyl)pyridazine in rats

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Summary

The purpose of the study was to investigate the in vivo metabolic pathway of 3-oxo-5-benzylidene-6-methyl-(4H)-2-(benzoylmethyl)pyridazine (substrate) in rats. Firstly its potential metabolites, i.e. N-dealkylation, ring scission of pyridazine and aromatic hydroxylation products, were synthesized and then the substrate was given orally (100 mg/kg) to male or female Wistar rats at a dose of 100 mg/kg to body weight. Blood samples were collected at 0, 1, 2, 4, 6 and 8 hours after administration of substrate and blood was centrifuged to obtain serum. The substrate and its potential metabolites were separated using a gradient HPLC method on a reverse phase system. This study revealed that 3-oxo-5-benzylidene-6-methyl-(4H)-2-(benzoylmethyl)pyridazine was not metabolized to the proposed metabolites and was present unchanged in the serum.

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Authors and Affiliations

  1. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Marmara University, 34668, Istanbul, Turkey

    E. Elçin Oruç & Sevim Rollas

  2. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Hacettepe University, Ankara, Turkey

    Oya Ünsal, AyLa Balkan & Fügen Özkanli

  3. Faculty of Medicine, Department of Pharmacology, Marmara University, Istanbul, Turkey

    M. Zafer Gören & Berna Terzioĝlu

Authors
  1. E. Elçin Oruç
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  2. Oya Ünsal
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  3. AyLa Balkan
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  4. Fügen Özkanli
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  5. M. Zafer Gören
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  6. Berna Terzioĝlu
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  7. Sevim Rollas
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Oruç, E.E., Ünsal, O., Balkan, A. et al. The in vivo metabolism of 3-oxo-5-benzylidene-6-methyl-(4H)-2-(benzoylmethyl)pyridazine in rats. European Journal of Drug Metabolism and Pharmacokinetics 31, 21–25 (2006). https://doi.org/10.1007/BF03190638

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  • DOI: https://doi.org/10.1007/BF03190638

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