NEL, New analogs of somatostatin: inhibiting effectively GH, glucagon and insulin levels

NeuroendocrinologyÝLetters incl. Psychoneuroimmunology & Chronobiology. Researh Papers. ISSNÝ0172ñ780X CopyrightÝ©Ý1999 NeuroendocrinologyÝLetters
Back	NEL VOL. 20 3/4 ORIGINAL ARTICLE	1999; 20:237–244
New analogs of somatostatin: inhibiting effectively GH, glucagon and insulin levels by Boguslawa Baranowska, Malgorzata Radzikowska, Elzbieta Wasilewska-Dziubinska, Artur Plonowski, Krzysztof Roguski, Anna Legowska & JÛzef Przybylski Key words: somatostatin analogs, growth hormone, insulin, glucagon Abstract The in vivo effects of three new analogs of somatostatin (ASS-51, ASS-52 and ASS-53 analogs) on GH, insulin and glucagon were studied in WKY rats. The solid phase method was used for the synthesis of ASS. Octreotide and ASS were given iv. in a dose of 0.05 µg/kg per animal in a time-dependent manner. ASS-52 and ASS-53 were longer acting and more potent somatostatin analogs when compared to octreotide in producing the inhibition of GH. ASS-51 was found to be the most potent and selective inhibitor of insulin and glucagon release. Our results show that the increased inhibitory effect and the higher selectivity of the new somatostatin analogs may result from the differences in their chemical structure. ASS-52 is most active in inhibiting GH release. The mechanism by which ASS-52 inhibits preferentially GH release may involve the opioid system and the activation of GABA-ergic receptors. In studies in vitro ASS-52 inhibited GH release from pituitary cells’ culture.
__________________________________________________________ Copyright © Neuroendocrinology Letters 1999 All rights reserved. No part may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, recording, or ortherwise, without prior written permission from the Editor-in-Chief.