Blog
About

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

      Effect of H-8, an Isoquinolinesulfonamide Inhibitor of Cyclic Nucleotide-Dependent Protein Kinase, on cAMP- and cGMP-Mediated Vasorelaxation

      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

          We theorized that H-8, N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide, an inhibitor of cyclic nucleotide-dependent protein kinases, might be a useful probe to assess cyclic nucleotide-dependent relaxation of blood vessels. However, working in the rat caudal artery and aorta, we found that neither cyclic AMP- nor cyclic GMP-mediated relaxations were diminished by even large doses of H-8. For example, in the caudal artery, relaxation of a phenylephrine contraction by 8-bromo-cGMP (10<sup>–5</sup> M) was unaffected by H-8: control, 33 ± 6.2%; 10 µ M H-8, 41 ± 12%; 30 µ M H-8, 30 ± 16% (p NS). The amount of relaxation by 8-bromo-cAMP (3 × 10<sup>–4</sup> M) was actually increased by H-8: control, 29 ± 7.6%; 10 µ M H-8, 34 ± 7.4%; 30 µ M H-8, 80 ± 14%. In the rat aorta, H-8 also failed to diminish relaxation induced by 8-bromo-cGMP, or by atriopeptin II or sodium nitroprusside. In both caudal artery and aorta, H-8 of itself caused a dose-dependent suppression of α-adrenergic contraction: for example, in the caudal artery, with 10 or 30 µ M H-8, peak contraction to phenylephrine was reduced to 70 (SEM) ± 12% or 52 ± 7% of control, respectively. The results suggest that the protein kinase inhibitor H-8 is not a useful probe to study cyclic nucleotide-dependent relaxation.

          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
          1991
          1991
          23 September 2008
          : 28
          : 5
          : 366-371
          Affiliations
          Department of Medicine, University of Illinois at Chicago School of Medicine and Westside V.A. Medical Center, Chicago, Ill.; Department of Physiology, Loyola University School of Medicine, Maywood, Ill, USA
          Article
          158883 Blood Vessels 1991;28:366–371
          10.1159/000158883
          © 1991 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: 6
          Categories
          Research Paper

          Comments

          Comment on this article