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The novel high-affinity antagonist, galantide, blocks the galanin-mediated inhibition of glucose-induced insulin secretion

Academic Article
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Overview

authors

  • Lindskog, S.
  • Ahren, B.
  • Land, T.
  • Langel, Ülo
  • Bartfai, Tamas

publication date

  • January 1992

journal

  • European Journal of Pharmacology  Journal

abstract

  • This study describes the synthesis and effects of the first antagonist to the widely distributed neuropeptide, galanin, which inhibits the secretion of insulin. The first galanin antagonist is a 20-amino acid-long chimeric peptide of the composition galanin-(1-12)-Pro-substance P-(5-11) amide: Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Gln-Gln-Phe-Phe-Gly- Leu-Met amide. The peptide dose dependently (IC50 = 1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. The antagonist was also found to displace 125I-monoiodo-[Tyr26]galanin from membranes of the insulin producing Rin m 5F cells with an IC50 value of less than 0.1 nM. The antagonist is named galantide.

subject areas

  • Amino Acid Sequence
  • Animals
  • Cell Membrane
  • Cells, Cultured
  • Female
  • Galanin
  • Glucose
  • Insulin
  • Iodine Radioisotopes
  • Islets of Langerhans
  • Mice
  • Mice, Inbred Strains
  • Molecular Sequence Data
  • Neuropeptides
  • Peptides
  • Receptors, Galanin
  • Receptors, Gastrointestinal Hormone
  • Subcellular Fractions
  • Substance P
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Research

keywords

  • (DISPLACEMENT)
  • GALANIN
  • GALANIN RECEPTOR ANTAGONISTS
  • GALANTIDE
  • INSULIN SECRETION
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Identity

International Standard Serial Number (ISSN)

  • 0014-2999

Digital Object Identifier (DOI)

  • 10.1016/0014-2999(92)90669-u

PubMed ID

  • 1376272
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Additional Document Info

start page

  • 183

end page

  • 188

volume

  • 210

issue

  • 2

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