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Vol. 76, No. 4, 2002
Issue release date: October 2002
Section title: Central Effects of Estrogens and Reproductive Neuroendocrinology
Neuroendocrinology 2002;76:214–222
(DOI:10.1159/000065951)

Estrogenic Properties of Raloxifene, but Not Tamoxifen, on D2 and D3 Dopamine Receptors in the Rat Forebrain

Landry M. · Lévesque D. · Di Paolo T.
aMolecular Endocrinology and Oncology Research Center and Faculté de Pharmacie, bUnité de Neuroscience, Centre de Recherche du CHUQ and Département de Médecine, Faculté de Médecine, Université Laval, Sainte-Foy, Que., Canada

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Article / Publication Details

First-Page Preview
Abstract of Central Effects of Estrogens and Reproductive Neuroendocrinology

Accepted: 1/29/2002
Published online: 10/31/2002

Number of Print Pages: 9
Number of Figures: 5
Number of Tables: 1

ISSN: 0028-3835 (Print)
eISSN: 1423-0194 (Online)

For additional information: http://www.karger.com/NEN

Abstract

The present study investigated the estrogenic specificity of the modulation of dopamine D2 and D3 receptors by comparing the effects of estradiol with tamoxifen or raloxifene. These compounds have estrogenic and/or antiestrogenic activity depending on the target tissue. Two weeks after ovariectomy of female rats, we observed a 60% decrease in the uterine weight, which was prevented by a replacement therapy of 2 weeks with 17β-estradiol. A tamoxifen or raloxifene treatment of 2 weeks increased uterine weights by 35 and 15%, respectively, but significantly less than estradiol treatment. Ovariectomy decreased dopamine D2 receptor specific binding (20%) in the dorsolateral part of the anterior striatum and these receptors were left unchanged in the other parts of the striatum as well as in the olfactory tubercle and the nucleus accumbens. 17β-Estradiol and raloxifene, but not tamoxifen treatment prevented this decrease. Ovariectomy left dopamine D3 receptor specific binding unchanged. However, estradiol and raloxifene treatment decreased dopamine D3 receptor binding in the islands of Calleja, the core and shell of the nucleus accumbens and the dorsal part of the anterior striatum, compared with ovariectomized rats. Our results show that raloxifene, but not tamoxifen, has an agonist estrogenic activity on dopamine receptors. Furthermore, estradiol and raloxifene have opposite effects on specific binding to dopamine D2 and D3 receptors.


Article / Publication Details

First-Page Preview
Abstract of Central Effects of Estrogens and Reproductive Neuroendocrinology

Accepted: 1/29/2002
Published online: 10/31/2002

Number of Print Pages: 9
Number of Figures: 5
Number of Tables: 1

ISSN: 0028-3835 (Print)
eISSN: 1423-0194 (Online)

For additional information: http://www.karger.com/NEN


Copyright / Drug Dosage

Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher or, in the case of photocopying, direct payment of a specified fee to the Copyright Clearance Center.
Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in goverment regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

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