Raloxifene and estradiol benzoate both fully restore hippocampal choline acetyltransferase activity in ovariectomized rats

Brain Research

Volumn 847, Issue 1, 1999, Pages 98-104

  Wu, Xin ^a   Glinn, Michele A ^a   Ostrowski, Nancy L ^a   Su, Yuan ^a   Ni, Binhui ^a   Cole, Harlan W ^a   Bryant, Henry U ^a   Paul, Steven M ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Choline acetyltransferase activity; Estrogen; Hippocampus; Raloxifene

Indexed keywords

CHOLINE ACETYLTRANSFERASE; ESTRADIOL BENZOATE; ESTROGEN RECEPTOR; RALOXIFENE; TAMOXIFEN;

ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRAIN REGION; CONTROLLED STUDY; DOSE RESPONSE; ENZYME ACTIVITY; FEMALE; HIPPOCAMPUS; HYPOTHALAMUS; NONHUMAN; OVARIECTOMY; PRIORITY JOURNAL; RAT; SUBCUTANEOUS DRUG ADMINISTRATION; UTERUS WEIGHT;

ALZHEIMER DISEASE; ANIMALS; CHOLINE O-ACETYLTRANSFERASE; DOSE-RESPONSE RELATIONSHIP, DRUG; ESTRADIOL; FEMALE; HIPPOCAMPUS; OVARIECTOMY; RALOXIFENE; RATS; RATS, SPRAGUE-DAWLEY; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 0032749899     PISSN: 00068993     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-8993(99)02062-4     Document Type: Article

References (41)

1. Barkhem T., Carlsson B., Nilsson Y., Enmark E., Gustafsson J.-A., Nilsson S. Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists. Mol. Pharmacol. 54:1998;105-112.
2. Black L.J., Sato M., Rowley E.R., Magee D.E., Bekele A., Williams D.C., Cullinan G.J., Bendele R., Kauffman R.F., Bensch W.R.et al. Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J. Clin. Invest. 93:1994;63-69.
3. Bowen D.M., Smith C.B., White P., Flack R.H., Carrasco L.H., Gedye J.L., Davison A.N. Chemical pathology of this organic dementias: II. Quantitative estimation of cellular changes in post-mortem brains. Brain. 100:1977;427-453.
4. Bryant H.U., Dere W.H. Selective estrogen receptor modulators: an alternative to hormone replacement therapy. Proc. Soc. Exp. Biol. Med. 217:1998;45-52.
5. Ciocca D.R., Roig L.M. Estrogen receptors in human nontarget tissues: biological and clinical implications. Endocr. Rev. 16(1):1995;35-62.
6. Cohen I., Altaras M.M., Shapira J., Tepper R., Rosen D.J., Cordoba M., Zalel Y., Figer A., Yigael D., Beyth Y. Time-dependent effect of tamoxifen therapy on endometrial pathology in asymptomatic postmenopausal breast cancer patients. Int. J. Gynecol. Pathol. 15:1996;152-157.
7. Decker M.W., McGaugh J.L. The role of interactions between the cholinergic system and other neuromodulatory systems in learning and memory. Synapse. 7:1991;151-168.
8. Delmas P.D., Bjarnason N.H., Mitlak B.H., Ravoux A.C., Shah A.S., Huster W.J., Draper M., Christiansen C. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N. Engl. J. Med. 337(23):1997;1641-1647.
9. Flicker C., Dean R.L., Watkins D.L., Fisher S.K., Bartus R.T. Behavioral and neurochemical effects following neurotoxic lesions of a major cholinergic input to the cerebral cortex in the rat. Pharmacol. Biochem. Behav. 18:1983;973-981.
10. Gibbs R.B., Wu D., Hersh L.B., Pfaff D.W. Effects of estrogen replacement on the relative levels of choline acetyltransferase, trkA, and nerve growth factor messenger RNAs in the basal forebrain and hippocampal formation of adult rats. Exp. Neurol. 129:1994;70-80.
11. Gibbs R.B. Effects of estrogen on basal forebrain cholinergic neurons vary as a function of dose and duration of treatment. Brain Res. 757:1997;10-16.
12. Gize E.A., Venugopalan M., Glasebrook A.L., Yang N.N. Charaterization of raloxifene binding and transactivation properties of the estrogen receptor-beta (Erbeta) - ASBMR 19th Annual Metting. J. Bone Miner. Res. 12:1997;S460.
13. Honjo H., Tanaka K., Kashiwagi T., Urabe M., Okada H., Hayashi M., Hayashi K. Senile dementia-Alzheimer's type and estrogen. Horm. Metab. Res. 27:1995;204-207.
14. Jones C.D., Jevnikar M.G., Pike A.J., Peters M.K., Black L.J., Thompson A.R., Falcone J.F., Clemens J.A. Antiestrogens, structure-activity studies in a series of 3-aroyl-2-arylbenzo[b] thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl) benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]-phenyl] methanone hydrochloride (LY156758), are markably effective estrogen antagonist with only minimal intrinsic estrogenicity. J. Med. Chem. 27(8):1984;1057-1066.
15. Kuiper G.G., Carlsson B., Grandien K., Enmark E., Haggblad J., Nilsson S., Gustafsson J.A. Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology. 138:1997;863-870.
16. Laflamme N., Nappi R.E., Drolet G., Labrie C., Rivest S. Expression and neuropeptidergic characterization of estrogen receptors (ERalpha and ERbeta) throughout the rat brain: anatomical evidence of distinct roles of each subtype. J. Neurobiol. 36:1998;357-378.
17. Luine V.N. Estradiol increases choline acetyltransferase activity in specific basal forebrain nuclei and projection areas of female rats. Exp. Neurol. 89:1985;484-490.
18. McEwen B.S., Woolley C.S. Estradiol and progesterone regulate neuronal structure and synaptic connectivity in adult as well as developing brain. Exp. Gerontol. 29(3-4):1994;431-436.
19. McMillan P.J., Singer C.A., Dorsa D.M. The effects of ovariectomy and estrogen replacement on trkA and choline acetyltransferase mRNA expression in the basal forebrain of the adult female Sprague-Dawley rat. J. Neurosci. 16:1996;1860-1885.
20. Mitlak B.H., Cohen F.J. In search of optimal long-term female hormone replacement: the potential of selective estrogen receptor modulators. Horm. Res. 48:1997;155-163.
21. Muir J.L. Acetylcholine, aging, and Alzheimer's disease. Pharmacol. Biochem. Behav. 56:1997;687-696.
22. Nickelsen T., Lufkin E.G., Riggs B.L., Cox D.A., Crook T.H. Raloxifene hydrochloride, a selective estrogen receptor modulator: safety assessment of effects on cognitive function and mood in postmenopausal women. Psychoneuroendocrinology. 24:1998;115-128.
23. Nilsen J., Mor G., Naftolin F. Raloxifene induces neurite outgrowth in estrogen receptor positive PC12 cells. Menopause. 5:1998;211-216.
24. Nonner D., Barrett E.F., Barrett J.N. Neurotrophin effects on survival and expression of cholinergic properties in cultured rat septal neurons under normal and stress conditions. J. Neurosci. 16:1996;6665-6675.
25. Ohara T., Tanaka K., Fukaya H., Demura N., Iimura A., Seno N. SDZ ENA 713 facilitates central cholinergic function and ameliorates spatial memory impairment in rats. Behav. Brain Res. 83:1997;229-233.
26. Ohkura T., Isse K., Akazawa K., Hamamoto M., Yaoi Y., Hagino N. Evaluation of estrogen treatment in female patients with dementia of the Alzheimer type. Endocr. J. 41:1994;361-371.
27. Paganini-Hill A., Henderson V.W. Estrogen deficiency and risk of Alzheimer's disease in women. Am. J. Epidemiol. 140(3):1994;256-261.
28. Rice M.M., Graves A.B., McCurry S.M., Larson E.B. Estrogen replacement therapy and cognitive function in postmenopausal women without dementia. Am. J. Med. 103:1997;22.
29. Sato M., Rippy M.K., Bryant H.U. Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J. 10:1996;905-912.
30. Schneider L.S., Farlow M. Combined tacrine and estrogen replacement therapy in patients with Alzheimer's disease. Ann. N. Y. Acad. Sci. 826:1997;317-322.
31. Schoepp D.D., Salhoff C.R., Hillman C.C., Ornstein P.L. CGS-19755 and MK-801 selectively prevent rat striatal cholinergic and gabaergic neuronal degeneration induced by N-methyl-D-aspartate and ibotenate in vivo. J. Neural Transm.: Gen. Sec. 78:1989;183-193.
32. Shughrue P.J., Lane M.V., Merchenthaler I. Regulation of progesterone receptor messenger ribonucleic acid in the rat medial preoptic nucleus by estrogenic and antiestrogenic compounds: an in situ hybridization study. Endocrinology. 138:1997;5476-5484.
33. Simpkins J.W., Green P.S., Gridley K.E., Singh M., Rajakumar G. Role of estrogen replacement therapy in memory enhancement and the prevention of neuronal loss associated with Alzheimer's disease. Am. J. Med. 103:1997;22.
34. Singh M., Meyer E.M., Millard W.J., Simpkins J.W. Ovarian steroid deprivation results in a reversible learning impairment and compromised cholinergic function in female Sprague-Dawley rats. Brain Res. 644:1994;305-312.
35. Singh M., Meyer E.M., Simpkins J.W. The effect of ovariectomy and estradiol replacement on brain-derived neurotrophic factor messenger ribonucleic acid expression in cortical and hippocampal brain regions of female Sprague-Dawley rats. Endocrinology. 136:1995;2320-2324.
36. Tang M.X., Jacobs D., Stern Y., Marder K., Schofield P., Gurland B., Andrews H., Mayeux R. Effect of estrogen during menopause on risk and age at onset of Alzheimer's disease. Lancet. 348(9025):1996;429-432.
37. Wakeling A.E., Valcaccia B., Newboult E., Green L.R. Non-steroidal antioestrogens-receptor binding and biological response in rat uterus, rat mammary carcinoma and human breast cancer cells. J. Steroid Biochem. 20:1984;111-120.
38. Walsh B.W., Kuller L.H., Wild R.A., Paul S., Farmer M., Lawrence J.B., Shah A.S., Anderson P.W. Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women. JAMA. 279(18):1998;1445-1451.
39. Watters J.J., Dorsa D.M. Transcriptional effects of estrogen on neuronal neurotensin gene expression involve cAMP/protein kinase A-dependent signaling mechanisms. J. Neurosci. 18:1998;6672-6680.
40. Witt D.M., Lousberg T.R. Controversies surrounding estrogen use in postmenopausal women. Ann. Pharmacother. 31:1997;745-755.
41. Wu X., Glinn M., Su Y., Ni B., Cole H., Bryant H.U., Paul S.M. Raloxifene increases hippocampal choline acetyltransferase activity in ovariectomized rats. Soc. Neurosci. Abstr. 24:1998;732.