STS 557, a new orally active progestin with antiprogestational and contragestational properties in rabbits

Oettel, M; Kurischko, A.

doi:10.1016/0010-7824(80)90140-7

Cited by 28 publications

(4 citation statements)

References 4 publications

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“…We also recently observed photoproduct-to-parent reversion for dienogest, a potent progestin used as an oral contraceptive (22), and for dienedione, an illicit anabolic steroid marketed as a “bodybuilding supplement” (fig. S23).…”

mentioning

confidence: 96%

Product-to-Parent Reversion of Trenbolone: Unrecognized Risks for Endocrine Disruption

Kolodziej

Long

et al. 2013

Science

100

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Trenbolone acetate (TBA) is a high-value steroidal growth promoter often administered to beef cattle, whose metabolites are potent endocrine-disrupting compounds. We performed laboratory and field phototransformation experiments to assess the fate of TBA metabolites and their photoproducts. Unexpectedly, we observed that the rapid photohydration of TBA metabolites is reversible under conditions representative of those in surface waters (pH 7, 25°C). This product-to-parent reversion mechanism results in diurnal cycling and substantial regeneration of TBA metabolites at rates that are strongly temperature- and pH-dependent. Photoproducts can also react to produce structural analogs of TBA metabolites. These reactions also occur in structurally similar steroids, including human pharmaceuticals, which suggests that predictive fate models and regulatory risk assessment paradigms must account for transformation products of high-risk environmental contaminants such as endocrine-disrupting steroids.

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mentioning

confidence: 96%

Product-to-Parent Reversion of Trenbolone: Unrecognized Risks for Endocrine Disruption

Kolodziej

Long

et al. 2013

Science

100

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“…The impressive antifertility effect of STS 557 reported earlier for female and male rodents and/or rabbits (Oetteri and Kurischko, 1980;Freund et al, 1980;Schubert et al, 1980) and the high interceptive activity in the baboon (Oettel and Kurischko, 1980) contrast to the weak ability of this compound to suppress the LII secretion in the rat; STS 557 is about 15 times less active than levonorgestrel in this regard (Oettel et al, 1980 a). Since the highest post-coital contraceptive (interceptive) effect occurs in the pregnant rat when STS 557 is administered on day 1 or on days 1-4 of pregnancy but not on days 5- 8 (Strecke et al, 1983), it has been suggested that the early implantation phase is disturbed.…”

Section: Discussionmentioning

confidence: 74%

Influence of STS 557 on the Mitotic Activity in the Endometrium of Ovariectomized Mice and Comparison with the Effects of Progesterone and Levonorgestrel

Koch¹

2009

Exp Clin Endocrinol Diabetes

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The numbers of mitoses in the epithelial and stromal tissues of mouse uteri were recorded after treatment with various doses of progesterone (P), levonorgestrel (LN), and STS 557 (17 alpha-cyanomethyl-17 beta-hydroxy-estra-4,9(10)-diene-3-one). All three progestins induced mitotic activity in the stromal tissue of the endometrium in which P and LN were much more active than STS 557. While the cell divisions in the luminal and glandular epithelium induced by P were only rare, LN and STS 557 enhanced the mitosis rates in these tissues significantly at a daily dose of 1.0 mg/animal on 5 consecutive days. The results are discussed with special regard to the post-coital antifertility effect of STS 557.

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“…Dienogest was initially produced in 1979. It is a very potent progestin that also has antiandrogenic activity [30,31]. Chlormadinone acetate is a derivative of 17a-hydroxyprogesterone.…”

Section: Later Progestinsmentioning

confidence: 99%

Currently available combined oral contraception

Kimble

Thurman

Schwartz

2011

Expert Review of Obstetrics & Gynecology

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STS 557, a new orally active progestin with antiprogestational and contragestational properties in rabbits

Cited by 28 publications

References 4 publications

Product-to-Parent Reversion of Trenbolone: Unrecognized Risks for Endocrine Disruption

Product-to-Parent Reversion of Trenbolone: Unrecognized Risks for Endocrine Disruption

Influence of STS 557 on the Mitotic Activity in the Endometrium of Ovariectomized Mice and Comparison with the Effects of Progesterone and Levonorgestrel

Currently available combined oral contraception

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