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Horm Metab Res 1974; 6(3): 181-183
DOI: 10.1055/s-0028-1093868
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© Georg Thieme Verlag KG Stuttgart · New York

The Subcellular Distribution of 14C-Glibenclamide in Different Tissues of Rat

J.  Somogyi , I.  Vincze , F.  Willig , F. H. Schmidt
  • Experimental Research Department and 1st Department of Chemistry and Biochemistry, Semmelweis University Medical School Budapest, Hungary;
    1st Department of Medicine, Medical Faculty in Mannheim, University of Heidelberg, Mannheim and Research Laboratory for Metabolism of Boehringer Mannheim GmbH, Mannheim, Germany
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Publication Date:
08 January 2009 (online)

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Abstract

One hour after intraperitoneal administration of 50 µC/kg 14C-glibenclamide to the rats, ca. 70% of the total radioactivity of liver or kidney homogenate was localised in the cytoplasmic fraction. About 10% of the homogenate activity was detected in the nuclear as well as microsomal fractions, while ca. 5% was found in the mitochondrial fraction. When distribution of 14C-glibenclamide between particular and soluble fractions of various rat organs was examined (homogenates were centrifuged with 100,000 × g for 60 min), ca. 20-25% of the homogenate activity was represented in the particular fraction and 70-80% was detected in the soluble fraction of all tissue homogenates tested. No changes in subcellular distribution of glibenclamide could be detected when doses of the radioactive material or the time interval between the administration of substance and the decapitation of the rats had been varied.

About 90% of radioactivity of the cytoplasmic fraction could be removed by 72 hours dialysis. It may be supposed that the majority of the radioactive material is located in the not protein bound fraction.

Key words

HB 419-Glibenclamide - Rat Organs - Subcellular distribution

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