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Journal of Pharmacology And Experimental Therapeutics, Vol. 177, Issue 2, 468-473, 1971
Copyright © 1971 by American Society for Pharmacology and Experimental Therapeutics

THE METABOLISM OF ETHYNODIOL DIACETATE BY RAT AND HUMAN LIVER

R. I. FREUDENTHAL 1, C. E. COOK 1, J. FORTH 1, R. ROSENFELD 1, and MONROE E. WALL 1

1 Chemistry and Life Sciences Laboratory, Research Triangle Institute, Research Triangle Park, North Carolina

Ethynodiol diacetate is metabolized by both rat and human liver to a number of intermediary metabolites. The biotransformation reaction involved in the in vitro metabolism of ethynodiol diacetate include deacetylation, saturation of ring A, aromatization of ring A, formation of a 3-ketone and a Dgr6-bond formation. The absolute structure of these metabolites are presented. The intermediary metabolites of ethynodiol diacetate undergo further biotransformation to more polar end products. The failure to hydrolyze the polar metabolites with either sulfatases or beta-glucuronidases suggests that this fraction consists mainly of polyhydroxylated steroids.

Submitted on November 20, 1971
Accepted on February 1, 1971






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Copyright © 1971 by the American Society for Pharmacology and Experimental Therapeutics.