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Horm Metab Res 1973; 5(2): 101-105
DOI: 10.1055/s-0028-1093972
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© Georg Thieme Verlag KG Stuttgart · New York

The Fate of Mestranol (17α-Ethynylestradiol-3-Methyl Ether) in the Isolated Perfused Rat Liver

H. M. Bolt , H.  Remmer
  • Institute of Toxicology, University of Tübingen, Germany
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Publication Date:
07 January 2009 (online)

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Abstract

Mestranol acts as an estrogen in the organism only after demethylation by the microsomal mixed function oxidase of the liver to the hormonally active ethynylestradiol. In the isolated perfused rat liver the disappearance of [6,7-3H-] mestranol and the availability of tritiated ethynylestradiol have been studied to construct a model of the mestranol metabolism in this organ suitable for later studies on the pharmacokinetics of mestranol in humans. The fate of mestranol has been compared with the transformation of estradiol. Biliary metabolites of both mestranol and estradiol from the isolated perfused rat liver have been measured.

Key words

17α-Ethynylestradiol - Mestranol - Contraceptive Compounds - Isolated Perfused Rat Liver - Biliary Estrogen Metabolites