Covalent protein binding of a minor deramciclane metabolite in dog plasma

Research output: Contribution to journalArticle

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 - 1998

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Protein Binding
Dogs
Camphor
Serum Albumin
Oral Administration
Half-Life
Blood Proteins
Mass Spectrometry
deramciclane
Therapeutics

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

Cite this

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title = "Covalent protein binding of a minor deramciclane metabolite in dog plasma",
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.",
author = "J. Visy and I. Fitos and G. M{\'a}dy and M. Simonyi and K. Lud{\'a}nyi and J{\'o}zsef Szunyog and I. Klebovich",
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T1 - Covalent protein binding of a minor deramciclane metabolite in dog plasma

AU - Visy, J.

AU - Fitos, I.

AU - Mády, G.

AU - Simonyi, M.

AU - Ludányi, K.

AU - Szunyog, József

AU - Klebovich, I.

PY - 1998

Y1 - 1998

N2 - 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.

AB - 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.

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