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

Oruc E., Unsal O., Balkan A., Ozkanli F., Goren M., TERZİOĞLU BEBİTOĞLU B., ...More

EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS, vol.31, no.1, pp.21-25, 2006 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 31 Issue: 1
  • Publication Date: 2006
  • Doi Number: 10.1007/bf03190638
  • Journal Name: EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.21-25
  • Keywords: 3-oxopyridazine, in vivo metabolism, rat serum, EBASTINE
  • Hacettepe University Affiliated: Yes

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, ling 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.