In vitro metabolism of gestodene in target organs: Formation of A-ring reduced derivatives with oestrogenic activity

European Journal of Pharmacology

Volumn 417, Issue 3, 2001, Pages 249-256

  Lemus, Ana E ^a   Santillán, René ^a   Damián Matsumura, Pablo ^b   García, Gustavo A ^c   Grillasca, Ivonne ^c   Pérez Palacios, Gregorio ^d  

^a INSTITUTO NACIONAL DE CIENCIAS MÉDICAS Y NUTRICIÓN SALVADOR ZUBIRÁN   (Mexico)

^b DEPARTAMENTO DE QUÍMICA   (Mexico)

^c UNIVERSIDAD NACIONAL AUTÓNOMA DE MÉXICO   (Mexico)

^d HOSPITAL GENERAL DE MÉXICO   (Mexico)

Author keywords

Gestodene 5 reduction; Gestodene metabolism; Oestrogenic effect; Synthetic progestin

Indexed keywords

3ALPHA,5ALPHA TETRAHYDROGESTODENE; 3BETA,5ALPHA TETRAHYDROGESTODENE; 5ALPHA DIHYDROGESTODENE; CARBON 14; DRUG METABOLITE; ESTROGEN; ESTROGEN RECEPTOR; GESTAGEN; GESTODENE; TRITIUM; UNCLASSIFIED DRUG;

ADENOHYPOPHYSIS; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BIOTRANSFORMATION; BREAST CANCER; DRUG METABOLISM; ESTROGEN ACTIVITY; FEMALE; HORMONAL CONTRACEPTION; HYPOTHALAMUS; MALE; NONHUMAN; PRIORITY JOURNAL; PROSTATE VENTRAL LOBE; RAT; RECEPTOR BINDING; TUMOR GROWTH;

ANIMALS; BIOTRANSFORMATION; CONTRACEPTIVES, ORAL, SYNTHETIC; FEMALE; HYDROGEN-ION CONCENTRATION; HYPOTHALAMUS; MALE; NADP; NORPREGNENES; PITUITARY GLAND, ANTERIOR; PROGESTERONE CONGENERS; PROSTATE; RATS; RATS, WISTAR; TESTOSTERONE; TESTOSTERONE 5-ALPHA-REDUCTASE;

EID: 0035853441     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(01)00893-7     Document Type: Article

References (31)

1. The androgenic, antiandrogenic and synandrogenic actions of progestins
2. A rapid and sensitive method for the quantitation of microgram quantities of protein utilising the principle of protein-dye binding
3. Molecular mechanisms of the antihormonal and antiimplantation effects of norethisterone and its A-ring reduced metabolites
4. Norgestrel and gestodene stimulate breast cancer cell growth through an oestrogen receptor mediated mechanism
5. Steroid metabolism in the mammalian brain: 5 alpha-reduction and aromatization
6. Stereospecificity of the intracellular binding of norethisterone and its A-ring reduced metabolites
7. Pharmacokinetics and biotransformation of gestodene in man
8. Risk of idiopathic cardiovascular death and nonfatal venous thromboembolism in women using oral contraceptives with differing progestagen components
9. Synthetic progestins induce proliferation of breast tumor cell lines via the progesterone or estrogen receptor
10. Mechanism of action of levonorgestrel: In vitro metabolism and specific interactions with steroid receptors in target organs
11. The oestrogenic effects of gestodene, a potent contraceptive progestin, are mediated by its A-ring reduced metabolites
12. The increased risk of venous thromboembolism and the use of third generation progestagens: Role of bias in observational research
13. 5α-reduced androgens play a key role in murine parturition
14. The transformation of testosterone into dihydrotestosterone by the brain and the anterior pituitary
15. Induction of male sexual behavior by norethisterone: Role of its A-ring reduced metabolites
16. Synandrogenic and antiandrogenic effect of progestins: Comparison with non-progestational antiandrogens
17. Tissue distribution and kinetic characteristics of rat steroid 5α-reductase isozymes
18. Estrogenic actions of norethisterone and its A-ring reduced metabolites. Induction of in vitro uterine sensitivity to serotonin
19. Norethisterone metabolites modulate the uteroglobin and progesterone receptor gene expression in prepubertal rabbits
20. Interaction of medroxyprogesterone acetate with cytosol androgen receptors in the rat hypothalamus and pituitary
21. Behavioral effects of synthetic progestins
22. Transient expression of the 5α-reductase type 2 isozyme in the rat brain in late fetal and early postnatal life
23. Steroid 5α-reductase: Two genes/two enzymes
24. Effects of two classes of progestagens, pregnane and 19-nortestosterone derivatives, on cell growth of human breast tumor cells: I. MCF-7 cell lines
25. Single dose phamacokinetics of gestodene in women after intravenous and oral adminstration
26. Characterization of Chinese hamster ovary cell lines expressing human steroid 5α-reductase isozymes
27. Effects of progestins on the proliferation of estrogen-dependent human breast tumor cells under growth factor-defined conditions
28. Evidence that a non-aromatizable metabolite of norethisterone induces estrogen-dependent pituitary progestin receptors
29. Metabolism of gestodene in human liver cytosol and microsomes in vitro
30. Venous thromboembolic disease and combined oral contraceptives: Results of international multicentre case-control study
31. Effect of different progestagens in low oestrogen oral contraceptives on venous thromboembolic disease