Abstract
The metabolic fate of labeled 18-homoestriol was investigated in man, dogs, and rats. In humans, urinary excretion values ranged from 9.5 to 26.4%. Two glucuronide conjugates of 18-homoestriol and small amounts of unchanged drug comprised most of the urinary radioactivity. In the dog and rat, urinary excretioh was also the minor route; however, more extensive biotransformations occurred. In rat urine, unchanged drug, 2-hydroxy-18-homoestriol, 16α-hydroxy-18-homoestrone, and three polar metabolites were found either before or after enzymatic cleavage of conjugates. In addition, dogs excreted large amounts of glucuronide and sulfate conjugates of 18-homoestriol as well as small amounts of unchanged drug. The use of DEAE-Sephadex A-25 permitted the separation of conjugated metabolites in dog and human urine.
Footnotes
- Received September 5, 1972.
- Copyright © 1973 by The American Society for Pharmacology and Experimental Therapeutics
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