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      Vasoactive Peptides and Their Receptors

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          Abstract

          Peptides act as vasoconstrictors (for instance angiotensins, vasopressin) or vasodilators (the kinins, the neurokinins), both through direct activation of specific receptors in the vascular smooth muscles or indirectly through the release of other endogenous inhibitors of the vascular tone. Kinins and neurokinins as well as their multiple receptors have been analyzed in the present study to assess the possible contributions of peptides to vasodilatation. Kinin receptors, B<sub>1</sub> and B<sub>2</sub>, have been characterized, using new selective agonists and antagonists. B<sub>1</sub> and B<sub>2</sub> receptors appear to present in endothelium (B2) and in smooth muscles (B<sub>2</sub>, B<sub>1</sub>) of a variety of isolated vessels of the dog and the rabbit, where they subserve both stimulatory and inhibitory effects. Vasodilator inhibitory mechanisms depend on the release of the endothelium-relaxing factor and/or of prostanoids from the endothelium or the smooth muscles, especially in the dog renal vessels, where both B<sub>1</sub>and B<sub>2</sub> receptors appear to be involved in causing vasodilatation. B<sub>2</sub> receptors have also been shown to activate cardiovascular reflexes through a direct action on sensory fibers or on reflexogenic areas of the epicardium. Three types of receptors for neurokinins, namely NK-1, NK-2 and NK-3, have been identified by the use of naturally occurring peptides and of some analogues that act as selective agonists of a single receptor type. NK-1 receptors (particularly sensitive to substance P) have been shown to be present in endothelia where they promote the release of the endothelium relaxing factor, while NK-2 receptors (sensitive to neurokinin A) are found in the pulmonary artery of the rabbit and act directly to contract the smooth muscle. NK-3 receptors (sensitive to neurokinin B) may be present in the veins where they act as venoconstrictors, increasing also the vascular permeability. Thus, peptides and their receptors participate through various mechanisms in the regulation of vascular tone and peripheral blood flow.

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          Author and article information

          Journal
          JVR
          J Vasc Res
          10.1159/issn.1018-1172
          Journal of Vascular Research
          S. Karger AG
          978-3-8055-5330-8
          978-3-318-01614-7
          1018-1172
          1423-0135
          1990
          1990
          23 September 2008
          : 27
          : 2-5
          : 137-145
          Affiliations
          Department of Pharmacology, Faculty of Medicine, University of Sherbrooke, Canada
          Article
          158804 Blood Vessels 1990;27:137–145
          10.1159/000158804
          © 1990 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: 9
          Categories
          Mechanisms of Vasodilatation

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