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      Specific α-Adrenergic Receptor Desensitization in Vascular Smooth Muscle


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          Specific desensitization of vascular tissue to norepinephrine was studied using an open-ring-type strip preparation of rabbit aorta. Aortae were taken from untreated, reserpine-pretreated (0.1 mg/kg/day; 3, 5, or 7 days) and 6-hydroxydopamine-pretreated (50 mg/kg; 3 or 7 days before sacrifice) rabbits. Aortic strips from the pretreated rabbits were supersensitive to norepinephrine. Subsequent to obtaining the first dose-response curve for norepinephrine, aortic strips were less sensitive to norepinephrine. It was found that desensitization to norepinephrine occurred following 10 min preincubation with 10<sup>–6</sup> m norepinephrine, and 20 min preincubation with 10<sup>–7</sup> m norepinephrine. The desensitization of supersensitive strips was significantly greater than in controls. Dopamine and isoproterenol desensitized both untreated and pretreated strips to norepinephrine. Phenylephrine desensitized strips to norepinephrine from 6-hydroxydopamine-pretreated rabbits. Acetylcholine and potassium did not desensitize strips to norepinephrine; however, acetylcholine desensitized strips to acetylcholine. It is concluded from these studies that norepinephrine desensitization is a specific α-adrenergic-related event.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          18 September 2008
          : 15
          : 4
          : 247-258
          Department of Pharmacology, The University of Texas Health Science Center at San Antonio, San Antonio, Tex., and Institut für Pharmakologie, Christian-Albrechts-Universität, Kiel
          158170 Blood Vessels 1978;15:247–258
          © 1978 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.

          : 17 December 1976
          : 21 June 1977
          Page count
          Pages: 12

          General medicine,Neurology,Cardiovascular Medicine,Internal medicine,Nephrology
          Supersensitivity,Sympathomimetics,Vascular adrenergic receptor,6-Hydroxydopamine,Desensitization,Reserpine


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