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      Cell Nuclear Accumulation of Estrogen Receptors in Rat Brain and Pituitary Gland after Treatment with a Dopamine-β-Hydroxylase Inhibitor

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          Abstract

          In a recent experiment, it was found that the dopamine-β-hydroxylase inhibitor, U-14,624, decreases the concentration of cytosol progestin receptors in guinea pig hypothalamus and causes an increase in the concentration of nuclear progestin receptors. In this series of experiments, the possibility that similar effects would be seen in the rat estrogen receptor system in mediobasal hypothalamus and pituitary was tested. U-14,624 caused a time-dependent decrease in the concentration of cytosol estrogen receptors and increase in the concentration of nuclear estrogen receptors in both mediobasal hypothalamus and anterior pituitary gland in ovariectomized rats, both in the absence and presence of low levels of estradiol, as well as in ovariectomized-adrenalectomized rats. The nuclear estrogen receptors that accumulate after U-14,624 injection do not require incubation at 25 <sup>¤</sup>C to be assayed, suggesting that they are not occupied by an estradiol-like ligand. The nuclear estrogen receptors that accumulate after U-14,624 treatment are high affinity, with an apparent dissociation constant of approximately 0.1 nM U-14,624 does not compete with (<sup>3</sup>H)estradiol, in vitro, suggesting that it does not directly interact with estrogen receptors. These results suggest that under some conditions, inhibition of dopamine-β-hydroxylase causes a modification in unoccupied estrogen receptors so that they develop a higher affinity for cell nuclear components.

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          Author and article information

          Journal
          NEN
          Neuroendocrinology
          10.1159/issn.0028-3835
          Neuroendocrinology
          S. Karger AG
          0028-3835
          1423-0194
          1986
          1986
          28 March 2008
          : 42
          : 1
          : 44-50
          Affiliations
          Division of Neuroscience and Behavior, Department of Psychology, University of Massachusetts, Amherst, Mass., USA
          Article
          124247 Neuroendocrinology 1986;42:44–50
          10.1159/000124247
          3941758
          f60139fa-1943-45d3-8206-8417666a7586
          © 1986 S. Karger AG, Basel

          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. 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 government 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.

          History
          : 21 August 1984
          : 15 February 1985
          Page count
          Pages: 7
          Categories
          Original Paper

          Endocrinology & Diabetes,Neurology,Nutrition & Dietetics,Sexual medicine,Internal medicine,Pharmacology & Pharmaceutical medicine
          Noradrenergic system,Pituitary gland,Hypothalamus,Norepinephrine,Estrogen receptors,Dopamine-β-hydroxylase inhibitor, U-14,624

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