PMID: 3320552Jan 1, 1987Paper

The metabolism of 19-nor contraceptive progestins modulates their biological activity at the neuroendocrine level

Journal of Steroid Biochemistry
F LarreaG Pérez-Palacios

Abstract

In this communication, a series of studies from our laboratory dealing with the mechanism of action of 17 alpha-ethinyl derivatives of 19-nor testosterone are reviewed. The administration of norethisterone (NET) to long-term castrated female rats induces the nuclear translocation of pituitary estradiol receptors and is followed by some estrogenic-like effects at the hypothalamic-pituitary unit. It is established that an A-ring reduced metabolite of NET, the 3 beta,5 alpha-tetrahydro NET derivative, is responsible for the observed in vivo estrogenic effects of the parent compound. 3 beta,5 alpha-NET binds to the estrogen receptor and is efficient in inducing the pituitary estrogen-dependent progesterone receptor and in increasing the uterine weight in long-term castrated rats. Furthermore, administration of 3 beta,5 alpha-NET and the 5 alpha-reduced metabolite of NET (5 alpha-NET) are able to inhibit the release of gonadotropins in the castrated animal to a greater extent than NET. Moreover, pretreatment with tamoxifen, an estrogen binding site competitor, results in a significant diminution of the antigonadotropic potency of 3 beta,5 alpha-NET but not of the 5 alpha-NET, which is only inhibited by the administration of cyproter...Continue Reading

References

Nov 15, 1978·The Biochemical Journal·A KasidK R Laumas
Jun 1, 1986·Acta Endocrinologica·J Garza-FloresG Pérez-Palacios
Jan 1, 1985·Journal of Steroid Biochemistry·B A ChávezG Pérez-Palacios
Sep 19, 1970·Lancet·H Breuer
Jun 1, 1972·Journal of Steroid Biochemistry·W G StillwellR N Stillwell
Apr 1, 1984·Journal of Steroid Biochemistry·F LarreaG Pérez-Palacios
Jul 1, 1981·Acta Endocrinologica·G Pérez-PalaciosA Ulloa-Aguirre
Dec 1, 1981·Journal of Steroid Biochemistry·G Pérez-PalaciosA E Pérez
Aug 1, 1983·The Journal of Clinical Endocrinology and Metabolism·R L BarbieriK J Ryan
Jul 1, 1983·Journal of Steroid Biochemistry·M L ThieulantA Vessieres
Jun 1, 1982·The Journal of Endocrinology·C R ClarkF Naftolin
Jul 30, 1958·Annals of the New York Academy of Sciences·M X ZARROWA L CALDWELL

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Citations

Feb 1, 1993·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·S D BainM W Edwards
Nov 1, 1990·Pharmacology, Biochemistry, and Behavior·G MoralíG Pérez-Palacios
Jan 1, 1991·The Journal of Steroid Biochemistry and Molecular Biology·J Garza-FloresG Pérez Palacios
Mar 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·G Pérez-PalaciosA E Lemus
Sep 6, 2002·Pharmacology, Biochemistry, and Behavior·G MoralíG Pérez-Palacios
Feb 19, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Rocio García-BecerraFernando Larrea
Jan 1, 1997·The Journal of Steroid Biochemistry and Molecular Biology·A E LemusG Pérez-Palacios
Jun 25, 2016·Journal of Molecular Endocrinology·Silvia GiattiMarzia Pesaresi
Jun 3, 2000·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·T RabeS Prifti
Feb 13, 2001·The Journal of Steroid Biochemistry and Molecular Biology·W G SchoonenH J Kloosterboer
Jul 21, 2004·The Journal of Steroid Biochemistry and Molecular Biology·Rocio García-BecerraFernando Larrea

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