Covalent protein binding of a minor deramciclane metabolite in dog plasma

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Abstract

The plasma protein interaction of a slowly eliminated substance which could be detected even after three weeks (about 0.2% of dose) in the plasma of Beagle dogs after a single oral administration of 10 mg kg-1 radiolabelled deramciclane, was determined. The substance, which could not be removed by extraction or displacement, was a metabolite irreversibly bound to serum albumin. The covalent adduct formed during the first 24 h after treatment, reached a maximum concentration between 1 and 4 days, and had an elimination half-life of approximately 10 days. The metabolite was isolated and subjected to mass spectrometry, and identified as a deramciclane derivative having a carboxylate group on the camphor ring.

Original languageEnglish
Pages (from-to)587-590
Number of pages4
JournalPharmacy and Pharmacology Communications
Volume4
Issue number12
Publication statusPublished - Dec 1 1998

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ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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