Blog
About

0
views
0
recommends
+1 Recommend
1 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: found

      Affinities of Adrenergic Drugs for α 2-Adrenoceptors in Dog Saphenous Vein in Comparison with Those in Rat Brain or Human Platelets

      Read this article at

      ScienceOpenPublisher
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          The affinities of drugs for the postsynaptic α<sub>2</sub>-adrenoceptors in the dog saphenous vein were examined and compared with those in human platelets or in rat brain. The pA<sub>2</sub> or pD<sub>2</sub> values in the vein were determined in the presence of phenoxybenzamine. The pKi values (dissociation constant) of drugs for binding to α<sub>2</sub>-adrenoceptors in human platelets or in rat brain were determined by radioligand binding assay using <sup>3</sup>H-yohimbine (YOH) or <sup>3</sup>Hclonidine (CLO) as ligands. The binding of agonists to <sup>3</sup>H-YOH binding sites was carried out in the presence of GTP. The pA<sub>2</sub> or pD<sub>2</sub> values in the vein had a good correlation with pKi values for YOH sites but not with those for CLO sites in rat brain. The pKi values for YOH sites in human platelets had a good correlation with those for YOH sites in the brain or with pA<sub>2</sub> or pD<sub>2</sub> values in the vein. These results suggested that the affinities of adrenergic drugs for postsynaptic α<sub>2</sub>-adrenoceptors in the dog saphenous vein are similar to those in brain and in platelets, and it is probable that the adrenergic drugs produce their α<sub>2</sub>-adrenoceptor-mediated effects on vascular tissues primarily through binding to a low-affinity form of the α<sub>2</sub>-adrenoceptors.

          Related collections

          Author and article information

          Journal
          JVR
          J Vasc Res
          10.1159/issn.1018-1172
          Journal of Vascular Research
          S. Karger AG
          1018-1172
          1423-0135
          1985
          1985
          23 September 2008
          : 22
          : 3
          : 127-138
          Affiliations
          Department of Pharmacology, Hamamatsu University School of Medicine, Hamamatsu, Japan
          Article
          158590 Blood Vessels 1985;22:127–138
          10.1159/000158590
          © 1985 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.

          Page count
          Pages: 12
          Categories
          Research Paper

          Comments

          Comment on this article