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      Somatostatin Structure-Activity Studies in the Stomach

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          Abstract

          Somatostatin may inhibit gastric exocrine functions independent of blockade of gastrin secretion. In order to further investigate this suppressive effect, somatostatin derivatives were injected to cats bearing a cannulated gastric fistula under pentagastrin stimulation. Results showed that somatostatin-14 was more potent than somatostatin-28 in this particular model. Analogues with substituted residues exhibited a variable spectrum of actions on hormone release and gastric function. A cyclic pentapeptide was deprived of gastric or GH inhibitory properties whereas the related peptide with a benzyl-protecting group on Thr was only devoid of gastric effect. The octapeptide SMS 201-995 was described as a potent inhibitor of gastric secretion in comparison with natural somatostatin in rats and also in humans, but was unable to induce maximal suppression of acid output in the cat model. Differences in gastric effect of different derivatives could be explained on the basis of binding to a selective subset of receptors, since at least two binding sites have been identified in the stomach mucosa. Serial studies with short cyclic somatostatin should help to establish a clear relationship between peptide structure and inhibition of gastric secretion.

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          Author and article information

          Journal
          HRE
          Horm Res Paediatr
          10.1159/issn.1663-2818
          Hormone Research in Paediatrics
          S. Karger AG
          978-3-8055-4809-0
          978-3-318-01960-5
          1663-2818
          1663-2826
          1988
          1988
          28 November 2008
          : 29
          : 2-3
          : 79-82
          Affiliations
          aDepartment of Physiological Sciences, University of Newcastle upon Tyne, Medical School, Newcastle upon Tyne, UK; bDepartamento de Fisiologia Animal, Facultad de Veterinaria, Universidad de Santiago de Compostela, Spain; cDepartamento de Bioquimica, Facultad de Medicina, Universidad de Alcala de Henares, Spain; dPeptide Research, Department of Medicine, Tulane University Medical Center, New Orleans, USA
          Article
          180973 Horm Res 1988;29:79–82
          10.1159/000180973
          2900201
          3fc53e30-a6ee-444c-ae65-2f83b9c9026d
          © 1988 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
          Page count
          Pages: 4
          Categories
          Somatostatin: Recent Advances in Basic Research and Clinical Applications

          Endocrinology & Diabetes,Neurology,Nutrition & Dietetics,Sexual medicine,Internal medicine,Pharmacology & Pharmaceutical medicine
          Gastric acid secretion,Gastric inhibition,Somatostatin,Pepsin secretion,Stomach

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