Control of rat tail skin temperature regulation by estrogen receptor-beta selective ligand

Maturitas

Volumn 64, Issue 1, 2009, Pages 46-51

  Opas, Evan E ^a   Scafonas, Angela ^a   Nantermet, Pascale V ^a   Wilkening, Robert R ^a   Birzin, Elizabeth T ^a   Wilkinson, Hilary ^a   Colwell, Lawrence F ^a   Schaeffer, James M ^a   Towler, Dwight A ^a   Rodan, Gideon A ^a   Schmidt, Azriel ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

ERaKO; Estrogen receptor alpha; Estrogen receptor beta; Hormone replacement; Hot flushes; Tail skin temperature; Thermoregulation; Uterocalin; Uterus

Indexed keywords

4 BROMO 9A BUTYL 7 HYDROXY 1,2,9,9A TETRAHYDRO 3H FLUOREN 3 ONE; ESTRADIOL; ESTROGEN; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FLUORENE DERIVATIVE; NEUTROPHIL GELATINASE ASSOCIATED LIPOCALIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BODY WEIGHT; CONTROLLED STUDY; DRUG DOSE COMPARISON; DRUG EFFECT; ESTROGEN DEFICIENCY; FEMALE; NONHUMAN; OVARIECTOMY; RAT; SKIN TEMPERATURE; TAIL; THERMOREGULATION; UTERUS WEIGHT;

ANIMALS; BODY TEMPERATURE REGULATION; BODY WEIGHT; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FEMALE; FLUORENES; GENE EXPRESSION REGULATION; LIGANDS; LIPOCALINS; ORGAN SIZE; OVARIECTOMY; RATS; RATS, SPRAGUE-DAWLEY; SKIN TEMPERATURE; TAIL; UTERUS;

RATTUS;

EID: 69549118307     PISSN: 03785122     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.maturitas.2009.07.007     Document Type: Article

References (29)

1. Barton D., Loprinzi C., and Wahner-Roedler D. Hot flashes: aetiology and management. Drugs Aging 18 (2001) 597-606
2. Carpenter J.S., Andrykowski M.A., Cordova M., et al. Hot flashes in postmenopausal women treated for breast carcinoma: prevalence, severity, correlates, management, and relation to quality of life. Cancer 82 (1998) 1682-1691
3. Freedman R.R. Physiology of hot flashes. Am J Hum Biol 13 (2001) 453-464
4. Morimoto L.M., White E., Chen Z., et al. Obesity, body size, and risk of postmenopausal breast cancer: the Women's Health Initiative (United States). Cancer Causes Control 13 (2002) 741-751
5. Pradhan A.D., Manson J.E., Rossouw J.E., et al. Inflammatory biomarkers, hormone replacement therapy, and incident coronary heart disease: prospective analysis from the Women's Health Initiative observational study. JAMA 288 (2002) 980-987
6. Jordan V.C., Gapstur S., and Morrow M. Selective estrogen receptor modulation and reduction in risk of breast cancer, osteoporosis, and coronary heart disease. J Natl Cancer Inst 93 (2001) 1449-1457
7. Seeman E. Raloxifene. J Bone Miner Metab 19 (2001) 65-75
8. Delmas P.D., Ensrud K.E., Adachi J.D., et al. Efficacy of raloxifene on vertebral fracture risk reduction in postmenopausal women with osteoporosis: four-year results from a randomized clinical trial. J Clin Endocrinol Metab 87 (2002) 3609-3617
9. Davies G.C., Huster W.J., Lu Y., Plouffe L.J., and Lakshmanan M. Adverse events reported by postmenopausal women in controlled trials with raloxifene. Obstet Gynecol 93 (1999) 558-565
10. Perez D.G., Zahasky K.M., Loprinzi C.L., et al. Tamoxifen-associated hot flashes in women. Supportive Cancer Therapy 4 (2007) 152-156
11. Sawka C.A., Pritchard K.I., Shelley W., et al. A randomized crossover trial of tamoxifen versus ovarian ablation for metastatic breast cancer in premenopausal women: a report of the National Cancer Institute of Canada Clinical Trials Group (NCIC CTG) trial MA.1. Breast Cancer Res Treat 44 (1997) 211-215
12. Kuiper G.G., Carlsson B., Grandien K., et al. Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology 138 (1997) 863-870
13. Kuiper G.G., Enmark E., Pelto-Huikko M., Nilsson S., and Gustafsson J.A. Cloning of a novel receptor expressed in rat prostate and ovary. Proc Natl Acad Sci U S A 93 (1996) 5925-5930
14. Couse J.F., Lindzey J., Grandien K., Gustafsson J.A., and Korach K.S. Tissue distribution and quantitative analysis of estrogen receptor-alpha (ERalpha) and estrogen receptor-beta (ERbeta) messenger ribonucleic acid in the wild-type and ERalpha-knockout mouse. Endocrinology 138 (1997) 41613-41621
15. Hewitt S.C., Harrell J.C., and Korach K.S. Lessons in estrogen biology from knockout and transgenic animals. Annu Rev Physiol 67 (2005) 285-308
16. Opas E.E., Gentile M.A., Kimmel D.B., Rodan G.A., and Schmidt A. Estrogenic control of thermoregulation in ERalphaKO and ERbetaKO mice. Maturitas 53 (2006) 210-216
17. Harris H.A., Katzenellenbogen J.A., and Katzenellenbogen B.S. Characterization of the biological roles of the estrogen receptors, ERalpha and ERbeta, in estrogen target tissues in vivo through the use of an ERalpha-selective ligand. Endocrinology 143 (2002) 4172-4177
18. Bowe J., Li X.F., Kinsey-Jones J., et al. The hop phytoestrogen, 8-prenylnaringenin, reverses the ovariectomy-induced rise in skin temperature in an animal model of menopausal hot flushes. J Endocrinol 191 (2006) 399-405
19. Wilkening R., Ratcliffe R., Tynebor E., et al. The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands. Bioorg Med Chem Lett 16 (2006) 3489-3494
20. Opas E.E., Rutledge S.J., Vogel R.L., Rodan G.A., and Schmidt A. Rat tail skin temperature regulation by estrogen, phytoestrogens and tamoxifen. Maturitas 48 (2004) 463-471
21. Scafonas A., Reszka A.A., Kimmel D.B., et al. Agonist-like SERM effects on ERalpha-mediated repression of MMP1 promoter activity predict in vivo effects on bone and uterus. J Steroid Biochem Mol Biol 110 (2008) 197-206
22. Wilkinson H.A., Dahllund J., Liu H., et al. Identification and characterization of a functionally distinct form of human estrogen receptor beta. Endocrinology 143 (2002) 1558-1561
23. Ernst M., Parker M.G., and Rodan G.A. Functional estrogen receptors in osteoblastic cells demonstrated by transfection with a reporter gene containing an estrogen response element. Mol Endocrinol 5 (1991) 1597-1606
24. Johnson T.E., Vogel R., Rutledge S.J., Rodan G., and Schmidt A. Thiazolidinedione effects on glucocorticoid receptor-mediated gene transcription and differentiation in osteoblastic cells. Endocrinology 140 (1999) 3245-3254
25. Krege J.H., Hodgin J.B., Couse J.F., et al. Generation and reproductive phenotypes of mice lacking estrogen receptor beta. Proc Natl Acad Sci U S A 95 (1998) 15677-15682
26. Nantermet P.V., Masarachia P., Gentile M.A., et al. Androgenic induction of growth and differentiation in the rodent uterus involves the modulation of estrogen-regulated genetic pathways. Endocrinology (2004)
27. Morrison S.F., Nakamura K., and Madden C.J. Central control of thermogenesis in mammals. Exp Physiol 93 (2008) 773-797
28. Deecher D.C. Physiology of thermoregulatory dysfunction and current approaches to the treatment of vasomotor symptoms. Expert Opin Invest Drugs 14 (2005) 435-448
29. Malamas M.S., Manas E.S., McDevitt R.E., et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem 47 (2004) 5021-5040