Inhibition of brain oestrogen receptors by RU 58668

Journal of Neuroendocrinology

Volumn 9, Issue 10, 1997, Pages 797-800

  Vagell, Michael E ^a   McGinnis, Marilyn Y ^a  

^a CITY UNIVERSITY OF NEW YORK   (United States)

Author keywords

Antagonist; Antioestrogen; Nuclear exchange assay; Pituitary; Progesterone receptor

Indexed keywords

11 [4 [[5 [(4,4,5,5,5 PENTAFLUOROPENTYL)SULFONYL]PENTYL]OXY]PHENYL]ESTRADIOL; ANTIESTROGEN; ESTRADIOL; ESTROGEN RECEPTOR; PROGESTERONE RECEPTOR; PROMEGESTONE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; BRAIN; BRAIN TISSUE; CELL NUCLEUS; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; FEMALE; HYPOPHYSIS; HYPOPHYSIS CELL; HYPOTHALAMUS; NONHUMAN; OVARIECTOMY; PRIORITY JOURNAL; RAT; SUBCUTANEOUS DRUG ADMINISTRATION;

EID: 0030766922     PISSN: 09538194     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2826.1997.d01-1047.x     Document Type: Article

References (38)

1. Wolf DM, Fuqua SA. Mechanisms of action of antiestrogens. Cancer Treat Rev 1995; 21: 247-271.
2. Jordan CV. Biochemical pharmacology of antiestrogen action. Pharm Rev 1984; 36: 245-276.
3. Hedden A, Muller V, Jensen EV. A new interpretation of antiestrogen action. Ann NY Acad Sci 1995; 761: 109-120.
4. Van de Velde P, Nique F, Bouchoux F, Bremaud J, Hameau MC, Lucas D, Moratille C, Viet S, Philibert D, Teutsch G. RU 58668, a new pure antiestrogen inducing a regression of human mammary carcinoma implanted in nude mice. J Steroid Biochem Mol Biol 1994; 48: 187-196.
5. Nique F, Van de Velde P. RU 58668, antineoplastic pure antiestrogen. Drugs Fut 1995; 20: 362-366.
6. Wakeling AE, Bowler J. Novel antiestrogens without partial agonist activity. J Steroid Biochem Molec Biol 1988; 31: 645-653.
7. Wakeling AE, Bowler J. ICI 182780, a new antiestrogen with clinical potential. J Steroid Biochem Molec Biol 1992; 43: 173-177.
8. Jin L, Borras M, Lacroix M, Legros N, Leclercq G. Antiestrogenic activity of two 11 beta-estradiol derivatives on MCF-7 breast cancer cells. Steroids 1995; 60: 512-518.
9. Van de Velde P, Nique F, Bremaud J, Hameau MC, Philibert D, Teutsch G. Exploration of the therapeutic potential of the antiestrogen RU 58668 in breast cancer treatment. Ann NY Acad Sci 1995; 761: 164-175.
10. Montagne MN, Dussaillant M, Chew LJ, Berod A, Lamberts SJ, Carter DA, Rostene W. Estradiol induces vasoactive intestinal peptide and prolactin gene expression in the rat anterior pituitary independently of plasma prolactin levels. J Neuroendocrinol 1995; 7: 225-231.
11. Vagell ME, McGinnis MY. Effects of the antiestrogen, RU 58668, on female sexual behavior in rats. Brain Res Bull 1996; 41: 121-124.
12. Pardridge WM, Mietus LJ. Transport of steroid hormones through the rat blood-brain barrier. Primary role of albumin-bound hormone. J Clin Invest 1979; 64: 145-154.
13. Wade GN, Blaustein JD, Gray JM, Meredith JM. ICI, 182,780: a pure antiestrogen that effects behaviors and energy balance in rats without acting on the brain. Am J Physiol 1993; 265: R1392-1398.
14. Roy EJ, McEwen BS. An exchange assay for estrogen receptors in the cell nuclei of the adult rat brain. Steroids 1977; 30: 657-669.
15. Roy EJ, MacLusky NJ, McEwen BS. Antiestrogen inhibits the induction of progestin receptors by estradiol in the hypothalamus-preoptic area and pituitary. Endocrinology 1979; 104: 1333-1336.
16. MacLusky NJ, McEwen BS. Progestin receptors in rat brain: distribution and properties of cytoplasmic progestin-binding sites. Endocrinology 1980; 106: 192-202.
17. Gorski J, Furlow JD, Murdoch FE, Fritsch M, Kaneko K, Ying C, Malayer JR. Perturbations in the model of estrogen receptor regulation of gene expression. Biol Reprod 1993; 48: 8-14.
18. Roy EJ, McEwen BS. Oestrogen receptors in cell nuclei of the hypothalamus-preoptic area-amygdala following an injection of oestradiol or the antiestrogen CI-628. J Endocrinol 1979; 83: 285-293.
19. Lustig RH, Mobbs CV, Bradlow HL, McEwen BS, Pfaff DW. Differential effects of estradiol and 16 alpha-hydroxyestrone on pituitary and preoptic estrogen receptor regulation. Endocrinology 1989; 125: 2701-2709.
20. Kirchhoff J, Hoffmann B, Ghraf R. Estrogen receptor translocation and replenishment in rat hypothalamus and pituitary gland after the application of catecholestrogen or nonsteroidal antiestrogen. J Steroid Biochem 1983; 18: 631-633.
21. Sica V, Weisz A, Petrillo A, Armetta I, Puca GA. Assay of total estradiol receptor in tissue homogenate and tissue fractions by exchange with sodium thiocyanate at low temperature. Biochemistry 1981; 20: 686-693.
22. Roy EJ. Antiestrogens and nuclear estrogen receptors in the brain. In: Current Studies of Hypothalamic Function, Basel: Karger, 1978: 204-213.
23. Leavitt WW, Okulicz WC. Progesterone control of nuclear estrogen receptor: demonstration in hamster uterus during the estrous cycle and pseudopregnancy using a new exchange assay. J Steroid Biochem 1985; 22: 583-588.
24. Krey LC, Kamel F, McEwen BS. Parameters of neuroendocrine aromatization and estrogen receptor occupation in the male rat. Brain Res 1980; 193: 277-283.
25. Anderson J, Clark JH, Peck Jr EJ. Oestrogen and nuclear binding sites. Biochem J 1972; 126: 561-567.
26. McGinnis MY, Krey LC, MacLusky NJ, McEwen BS. Steroid receptor levels in intact and ovariectomized estrogen-treated rats: an examination of quantitative, temporal and endocrine factors influencing the efficacy of an estradiol stimulus. Neuroendocrinology 1981; 33: 158-165.
27. Jordan VC, Dix CJ, Rowsby L, Prestwitch G. Studies on the mechanisms of action of the nonsteroidal antioestrogen tamoxifen (ICI 46474) in the rat. Moll Cell Endocrinol 1977; 7: 177-192.
28. Capony F, Rochefort H. In vivo effect of antiestrogens on the localization and replenishment of the estrogen receptor. Mol Cell Endocrinol 1975; 3: 233-251.
29. Pardridge WM. Steroid hormone transport through blood-brain barrier: Methods and concepts. In: Methods in Neurosciences, New York: Academic Press. 1994: 3-22.
30. Lauber AH, Romano GJ, Pfaff DW. Sex difference in estradiol regulation of progestin receptor mRNA in rat mediobasal hypothalamus as demonstrated by in situ hybridization. Neuroendocrinology 1991; 53: 608-613.
31. Etgen AM. Estrogen induction of progestin receptors in the hypothalamus of male and female rats which differ in their ability to exhibit cyclic gonadotropin secretion and female sexual behavior. Biol Reprod 1981; 25: 307-313.
32. Etgen AM, Shamamian P. Regulation of estrogen-stimulated lordosis behavior and hypothalamic progestin receptor induction by antiestrogens in female rats. Horm Behav 1986; 20: 166-180.
33. Clark CR, MacLusky NJ, Naftolin F. Oestrogen induction of progestin preceptors in the rat brain and pituitary gland: quantitative and kinetic aspects. J Endocr 1982; 93: 339-353.
34. Raynaud JP. R5020, a tag for the progestin receptor. In: Progesterone Receptors in Normal and Neoplastic Tissues, New York: Raven Press, 1977: 9-21.
35. Krey LC, McGinnis MY. Time-courses of the appearance/disappearance of nuclear androgen+ receptor complexes in the brain and adenohypophysis following testosterone administration withdrawal to castrated male rats: relationships with gonadotropin secretion. J Steroid Biochem 1990; 35: 403-408.
36. Burton K. A study of the conditions and mechanisms of the diphenylamine reaction for the colormetric estimation of DNA. Biochem J 1956; 62: 315-323.
37. Brown TJ, Clark AS, MacLusky NJ. Regional differences in progestin receptor induction in the rat hypothalamus: Effects of various doses of estradiol benzoate. J Neurosci 1987; 7: 2529-2536.
38. Bradford MM. A rapid and sensitive method for quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 1976; 72: 248-254.