INTERRUPTION OF PREGNANCY IN RATS BY VARIOUS FLUOROANDROSTANE DERIVATIVES

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Authors:
Y. TACHÉ
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J. TACHÉ
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DOI:
https://doi.org/10.1530/jrf.0.0390319
Volume/Issue:
Volume 39: Issue 2
Page Range:
319–327
Article Type:
Research Article
Online Publication Date:
Aug 1974
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Summary.

In the rat, pregnancy was affected by androstane derivatives (including three 9α-fluoro-4-androsten-3-one, 11-and 17-substituted), given orally in doses of 5 mg/100 g body weight from Days 3 to 10. Fluorohydroxyandrostenedione (FHA) and fluoxymesterone appeared to be 100% effective in suppressing fertility, while steroid U-6596 seriously disturbed gestation though not in all cases. Under similar experimental conditions, the abortifacient activity of FHA, fluoxymesterone and steroid U-6596 was respectively abolished, decreased or left unaltered after substitution of 9α-fluorine by hydrogen. The 5β-saturated homologues of FHA and fluoxymesterone, as well as 9α-fluoro-17α-methyl-5β-androstane-3α,11β,17-triol, were totally ineffective in interrupting pregnancy. The relative antifertility potency of the fluorosteroids in rats roughly paralleled their uterotrophic activity in immature mice.

Comparative studies showed that FHA (administered at the 5-mg dose level but from the 3rd to the 7th day of pregnancy) was more effective than the other two fluoroandrostenes tested. The abortifacient action of FHA was reduced when the dosage was decreased, the minimum 100% effective oral dose being 2·5 mg/100g body weight. In addition, this fluorosteroid also exerted some interceptive activity.

Progesterone abolished the abortifacient effect of 2·5, but not of 5 mg, of FHA. Under identical conditions, prolactin had no such protective influence.

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Print ISSN:
1470-1626
Online ISSN:
1741-7899