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Antidiabetic activity of a highly potent and selective nonpeptide somatostatin receptor subtype-2 agonist

Academic Article
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Overview

authors

  • Strowski, M. Z.
  • Cashen, D. E.
  • Birzin, E. T.
  • Yang, L. H.
  • Singh, V.
  • Jacks, T. M.
  • Nowak, K. W.
  • Rohrer, S. P.
  • Patchett, A. A.
  • Smith, Roy
  • Schaeffer, J. M.

publication date

  • October 2006

journal

  • Endocrinology  Journal

abstract

  • Somatostatin inhibits both glucagon and insulin secretion. Glucagon significantly contributes to hyperglycemia in type 2 diabetes. Despite its function in the inhibition of glucagon secretion, somatostatin fails to reduce hyperglycemia in type 2 diabetes, due to a parallel suppression of insulin secretion. Five pharmacologically distinct somatostatin receptor subtypes (sst(1)-sst(5)) mediate the effects of somatostatin on a cellular level. Pancreatic A cells express sst(2), whereas B cells express sst(5). In this study, we describe a novel approach to the treatment of type 2 diabetes using a highly sst(2)-selective, nonpeptide agonist (compound 1). Compound 1 effectively inhibited glucagon secretion from pancreatic islets isolated from wild-type mice, whereas glucagon secretion from sst(2)-deficient islets was not suppressed. Compound 1 did not influence nonfasted insulin concentration. In sst(2)-deficient mice, compound 1 did not have any effects on glucagon or glucose levels, confirming its sst(2) selectivity. In animal models of type 2 diabetes in the nonfasted state, circulating glucagon and glucose levels were decreased after treatment with compound 1. In the fasting state, compound 1 lowered blood glucose by approximately 25%. In summary, small-molecule sst(2)-selective agonists that suppress glucagon secretion offer a novel approach toward the development of orally bioavailable drugs for treatment of type 2 diabetes.

subject areas

  • Animals
  • Blood Glucose
  • Diabetes Mellitus, Type 2
  • Dogs
  • Glucagon
  • Growth Hormone
  • Hypoglycemic Agents
  • In Vitro Techniques
  • Insulin
  • Islets of Langerhans
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mice, Obese
  • Rats
  • Receptors, Somatostatin
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Identity

International Standard Serial Number (ISSN)

  • 0013-7227

Digital Object Identifier (DOI)

  • 10.1210/en.2006-0274

PubMed ID

  • 16857751
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Additional Document Info

start page

  • 4664

end page

  • 4673

volume

  • 147

issue

  • 10

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