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      Somatostatin Structure-Activity Studies in the Stomach

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          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

          Horm Res Paediatr
          Hormone Research in Paediatrics
          S. Karger AG
          28 November 2008
          : 29
          : 2-3
          : 79-82
          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
          180973 Horm Res 1988;29:79–82
          © 1988 S. Karger AG, Basel

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          Page count
          Pages: 4
          Somatostatin: Recent Advances in Basic Research and Clinical Applications


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