Literature DB >> 16715779

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

E Elçin Oruç1, Oya Unsal, Ayla Balkan, Fügen Ozkanli, M Zafer Gören, Berna Terzioğlu, Sevim Rollas.   

Abstract

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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Year:  2006        PMID: 16715779     DOI: 10.1007/BF03190638

Source DB:  PubMed          Journal:  Eur J Drug Metab Pharmacokinet        ISSN: 0378-7966            Impact factor:   2.441


  7 in total

1.  The in vitro hepatic metabolism of 1-phenyl-2-(2-benzothiazolinone-3-yl)ethanone and their reduced derivatives.

Authors:  F Yilmaz; M Ulgen; D S Doğruer; B Cakir; M F Sahin
Journal:  Exp Toxicol Pathol       Date:  1999-07

2.  Involvement of CYP2J2 and CYP4F12 in the metabolism of ebastine in human intestinal microsomes.

Authors:  Takanori Hashizume; Susumu Imaoka; Masashi Mise; Yoshiaki Terauchi; Toshihiko Fujii; Hisashi Miyazaki; Tetsuya Kamataki; Yoshihiko Funae
Journal:  J Pharmacol Exp Ther       Date:  2002-01       Impact factor: 4.030

3.  A novel cytochrome P450 enzyme responsible for the metabolism of ebastine in monkey small intestine.

Authors:  T Hashizume; M Mise; S Matsumoto; Y Terauchi; T Fujii; S Imaoka; Y Funae; T Kamataki; H Miyazaki
Journal:  Drug Metab Dispos       Date:  2001-06       Impact factor: 3.922

4.  The in vivo metabolism of 5-(4-nitrophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione in rats.

Authors:  E E Oruç; S Rollas; L Kabasakal; M K Uysal
Journal:  Drug Metabol Drug Interact       Date:  1999

5.  On the distribution and metabolism of azaperone (R 1929) in the rat and pig.

Authors:  J Heykants; L Pardoel; P A Janssen
Journal:  Arzneimittelforschung       Date:  1971-07

6.  In vivo metabolism of N-phenyl-N'-(3,5-dimethylpyrazole-4-yl) thiourea in rats.

Authors:  Bedia Koçyiğit Kaymakcioğlu; Sevim Rollas; Feyza Kartal-Aricioğlu
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2003 Oct-Dec       Impact factor: 2.441

7.  In vivo metabolism of 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene] hydrazide in rats.

Authors:  N N Gülerman; E E Oruç; F Kartal; S Rollas
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2000 Apr-Jun       Impact factor: 2.569

  7 in total

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