Analysis of the effects of oestrogen receptor α (ERα)- and ERβ-selective ligands given in combination to ovariectomized rats

British Journal of Pharmacology

Volumn 153, Issue 7, 2008, Pages 1432-1437

  Hertrampf, T ^a   Seibel, J ^a   Laudenbach, U ^a   Fritzemeier, K H ^b   Diel, P ^a,c  

^a GERMAN SPORT UNIVERSITY COLOGNE   (Germany)

^b BAYER PHARMA AG   (Germany)

^c Deutsche Sporthochschule Köln ^*  (Germany)

Author keywords

Oestrogen receptor; Oestrogens; Phytoestrogens; Running wheel activity

Indexed keywords

ESTRADIOL; ESTROGEN; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR ALPHA SPECIFIC AGONIST 16ALPHA LE2; ESTROGEN RECEPTOR BETA; ESTROGEN RECEPTOR BETA SPECIFIC AGONIST 8BETA VE2; FULVESTRANT; GENISTEIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BODY WEIGHT; BONE DENSITY; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG DOSE REDUCTION; DRUG EFFECT; DRUG STRUCTURE; FEMALE; NONHUMAN; OVARIECTOMY; PRIORITY JOURNAL; RAT; TREADMILL; WEIGHT GAIN;

ANIMALS; BODY WEIGHT; BONE DENSITY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG THERAPY, COMBINATION; ESTRADIOL; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; ESTROGENS; FEMALE; GENISTEIN; LIGANDS; MOTOR ACTIVITY; OVARIECTOMY; PHYTOESTROGENS; RATS; RATS, WISTAR;

EID: 41649114360     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707664     Document Type: Article

References (46)

1. Albertazzi P, Sharma S (2005). Urogenital effects of selective estrogen receptor modulators: a systematic review. Climacteric 8: 214-220.
2. Barkhem T, Carlsson B, Nilsson Y, Enmark E, Gustafsson J, Nilsson S (1998). Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists. Mol Pharmacol 54: 105-112.
3. Belcher SM, Zsarnovszky A (2001). Estrogenic actions in the brain: estrogen, phytoestrogens, and rapid intracellular signaling mechanisms. J Pharmacol Exp Ther 299: 408-414; review.
4. Cassidy A (2003). Potential risks and benefits of phytoestrogen-rich diets. Int J Vitam Nutr Res 73: 120-126; review.
5. Chen Z, Bassford T, Green SB, Cauley JA, Jackson RD, LaCroix AZ et al. (2005). Postmenopausal hormone therapy and body composition - a substudy of the estrogen plus progestin trial of the Women's Health Initiative. Am J Clin Nutr 82: 651-656.
6. Clark AS, Guarraci FA, Megroz AB, Porter DM, Henderson LP (2003). The display of sexual behaviors by female rats administered ICI 182,780. Horm Behav 43: 454-464. Erratum in: Horm Behav. 2004 46(4): 506.
7. Davis SR, Dalais FS, Simpson ER, Murkies AL (1999). Phytoestrogens in health and disease. Recent Prog Horm Res 54: 185-210; discussion 210-211. Review.
8. Deroo BJ, Korach KS (2006). Estrogen receptors and human disease. J Clin Invest 116: 561-570; review.
9. Diel P (2002). Tissue-specific estrogenic response and molecular mechanisms. Toxicol Lett 127: 217-224; review.
10. Diel P, Geis RB, Caldarelli A, Schmidt S, Leschowsky UL, Voss A et al. (2004). The differential ability of the phytoestrogen genistein and of estradiol to induce uterine weight and proliferation in the rat is associated with a substance specific modulation of uterine gene expression. Mol Cell Endocrinol 221: 21-32.
11. Fatehi M, Fatehi-Hassanabad Z (2007). Effects of 17beta-estradiol on neuronal cell excitability and neurotransmission in the suprachiasmatic nucleus of rat. Neuropsychopharmacology 30: 664-672.
12. Fitzpatrick LA (2003). Phytoestrogens-mechanism of action and effect on bone markers and bone minAlphal density. Endocrinol Metab Clin North Am 32: 233-252; review.
13. Garey J, Morgan MA, Frohlich J, McEwen BS, Pfaff DW (2001). Effects of the phytoestrogen coumestrol on locomotor and fear-related behaviors in female mice. Horm Behav 40: 65-76.
14. Gluck O, Maricic M (2003). Skeletal and nonskeletal effects of raloxifene. Curr Osteoporos Rep 1: 123-128; review.
15. Gustafsson JA (2000). An update on estrogen receptors. Semin Perinatol 24: 66-69; review.
16. Gustafsson JA (2003). What pharmacologists can learn from recent advances in estrogen signalling. Trends Pharmacol Sci 24: 479-485; review.
17. Gustafsson JA (2006). ERbeta scientific visions translate to clinical uses. Climacteric 9: 156-160.
18. Hegele-Hartung C, Siebel P, Peters O, Kosemund D, Muller G, Hillisch A et al. (2004). Impact of isotype-selective estrogen receptor agonists on ovarian function. Proc Natl Acad Sci USA 101: 5129-5134.
19. Hertrampf T, Degen GH, Kaid AA, Laudenbach-Leschowsky U, Seibel J, Di Virgilio AL et al. (2006). Combined effects of physical activity, dietary isoflavones and 17beta-estradiol on movement drive, body weight and bone mineral density in ovariectomized female rats. Planta Med 72: 484-487.
20. Hertrampf T, Gruca MJ, Seibel J, Laudenbach U, Fritzemeier KH, Diel P (2007). The bone-protective effect of the phytoestrogen Genistein is mediated via ERa-dependent mechanisms and strongly enhanced by physical activity. Bone 40: 1529-1535.
21. Hertrampf T, Schmidt S, Laudenbach-Leschowsky U, Seibel J, Diel P (2005). Tissue-specific modulation of cyclooxygenase-2 (Cox-2) expression in the uterus and the v. cava by estrogens and phytoestrogens. Mol Cell Endocrinol 243: 51-57.
22. Hillisch A, Peters O, Kosemund D, Muller G, Walter A, Schneider B et al. (2004). Dissecting physiological roles of estrogen receptor alpha and beta with potent selective ligands from structure-based design. Mol Endocrinol 18: 1599-1609.
23. Howell A, Osborne CK, Morris C, Wakeling AE (2000). ICI 182,780 (Faslodex): development of a novel, 'pure' antiestrogen. Cancer 89: 817-825. Erratum in: Cancer 2001 91(2): 455.
24. Kalu DN (1991). The ovariectomized rat model of postmenopausal bone loss. Bone Miner 15: 175-191; review.
25. Koehler KF, Helguero LA, Haldosen LA, Warner M, Gustafsson JA (2005). Reflections on the discovery and significance of estrogen receptor beta. Endocr Rev 26: 465-478; review.
26. Kuiper GG, Carlsson B, Grandien K, Enmark E, Haggblad J, Nilsson S et al. (1997). Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology 138: 863-870.
27. Kuiper GG, Enmark E, Pelto-Huikko M, Nilsson S, Gustafsson JA (1996). Cloning of a novel receptor expressed in rat prostate and ovary. Proc Natl Acad Sci USA 93: 5925-5930.
28. Kuiper GG, Lemmen JG, Carlsson B, Corton JC, Safe SH, van der Saag PT et al. (1998). Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta. Endocrinology 139: 4252-4263.
29. Mueller SO, Simon S, Chae K, Metzler M, Korach KS (2004). Phytoestrogens and their human metabolites show distinct agonistic and antagonistic properties on estrogen receptor alpha (ERalpha) and ERbeta in human cells. Toxicol Sci 80: 14-25. Erratum in: Toxicol Sci. 2004 Oct; 81(2): 530-531.
30. Ogawa S, Chan J, Gustafsson JA, Korach KS, Pfaff DW (2003). Estrogen increases running wheel activity in mice through estrogen receptor alpha: specificity for the type of activity. Endocrinology 144: 230-239.
31. Ohmichi M, Tasaka K, Kurachi H, Murata Y (2005). Molecular mechanism of action of selective estrogen receptor modulator in target tissues. Endocr J 52: 161-167; review.
32. Patisaul HB, Melby M, Whitten PL, Young LJ (2002). Genistein affects ER beta- but not ER alpha-dependent gene expression in the hypothalamus. Endocrinology 143: 2189-2197.
33. Pelzer T, Jazbutyte V, Hu K, Segerer S, Nahrendorf M, Nordbeck P et al. (2005). The estrogen receptor-alpha agonist 16alpha-LE2 inhibits cardiac hypertrophy and improves hemodynamic function in estrogen-deficient spontaneously hypertensive rats. Cardiovasc Res 67: 604-612.
34. Perez SE, Chen EY, Mufson EJ (2003). Distribution of estrogen receptor alpha and beta immunoreactive profiles in the postnatal rat brain. Brain Res Dev Brain Res 145: 117-139.
35. Pike AC, Brzozowski AM, Hubbard RE, Bonn T, Thorsell AG, Engstrom O et al. (1999). Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist. EMBO J 18: 4608-4618.
36. Plouffe Jr L (2000). Selective estrogen receptor modulators (SERMs) in clinical practice. J Soc Gynecol Investig 7 (1 Suppl): S38-S46; review.
37. Rocha BA, Fleischer R, Schaeffer JM, Rohrer SP, Hickey GJ (2005). 17 Beta-estradiol-induced antidepressant-like effect in the forced swim test is absent in estrogen receptor-beta knockout (BERKO) mice. Psychopharmacology (Berlin) 179: 637-643.
38. Scott CJ, Tilbrook AJ, Simmons DM, Rawson JA, Chu S, Fuller PJ et al. (2000). The distribution of cells containing estrogen receptor-alpha (ERalpha) and ERbeta messenger ribonucleic acid in the preoptic area and hypothalamus of the sheep: comparison of males and females. Endocrinology 141: 2951-2962.
39. Sorensen MB, Rosenfalck AM, Hojgaard L, Ottesen B (2001). Obesity and sarcopenia after menopause are reversed by sex hormone replacement therapy. Obes Res 9: 622-626.
40. Tanaka T, Shiina T, Hayashi S, Okamura H, Kamomae H, Kaneda Y (2003). Estrogen receptor alpha expression in the medial preoptic area and the medial basal hypothalamus under different physiological conditions in cattle. J Reprod Dev 49: 55-60.
41. Wade GN, Blaustein JD, Gray JM, Meredith JM (1993). ICI 182,780: a pure antiestrogen that affects behaviors and energy balance in rats without acting in the brain. Am J Physiol 265 (6 Part 2): R1392-R1398.
42. Walf AA, Frye CA (2005). ERbeta-selective estrogen receptor modulators produce antianxiety behavior when administered systemically to ovariectomized rats. Neuropsychopharmacology 30: 1598-1609.
43. Walf AA, Frye CA (2007). Administration of estrogen receptor beta-specific selective estrogen receptor modulators to the hippocampus decrease anxiety and depressive behavior of ovariectomized rats. Pharmacol Biochem Behav 86: 407-414.
44. Walf AA, Rhodes ME, Frye CA (2004). Antidepressant effects of ERbeta-selective estrogen receptor modulators in the forced swim test. Pharmacol Biochem Behav 78: 523-529.
45. Weihua Z, Andersson S, Cheng G, Simpson ER, Warner M, Gustafsson JA (2003). Update on estrogen signaling. FEBS Lett 546: 17-24.
46. Yokosuka M, Okamura H, Hayashi S (1997). Postnatal development and sex difference in neurons containing estrogen receptor-alpha immunoreactivity in the preoptic brain, the diencephalon, and the amygdala in the rat. J Comp Neurol 389: 81-93.