GLP-1 receptor antagonist as a potential probe for pancreatic β-cell imaging

Eri Mukai, Kentaro Toyoda, Hiroyuki Kimura, Hidekazu Kawashima, Hiroyuki Fujimoto, Masashi Ueda, Takashi Temma, Konomu Hirao, Kenji Nagakawa, Hideo Saji, Nobuya Inagaki

Research output: Contribution to journalArticlepeer-review

62 Citations (Scopus)


We examined exendin(9-39), an antagonist of glucagon-like peptide-1 (GLP-1) receptor (GLP-1R), as a potential probe for imaging of pancreatic β-cells. To evaluate in vitro receptor specificity, binding assay was performed using dispersed mouse islet cells. Binding assay showed competitive inhibition of [125I]BH-exendin(9-39) binding by non-radioactive exendin(9-39). To assess in vivo selectivity, the biodistribution was evaluated by intravenous administration of [125I]BH-exendin(9-39) to mice. Radioactivity of harvested pancreas reached highest levels at 60 and 120 min among organs examined except lung. Pre-administration of excess non-radioactive exendin(9-39) remarkably and specifically blocked the radioactivity of pancreas. After [125I]BH-exendin(9-39) injection into transgenic mice with pancreatic β-cells expressing GFP, fluorescent and radioactive signals of sections of pancreas were evaluated with an image analyzer. Imaging analysis showed that the fluorescent GFP signals and the radioactive signals were correspondingly located. Thus, the GLP-1R antagonist exendin(9-39) may serve as a useful probe for pancreatic β-cell imaging.

Original languageEnglish
Pages (from-to)523-526
Number of pages4
JournalBiochemical and Biophysical Research Communications
Issue number3
Publication statusPublished - Nov 2009
Externally publishedYes


  • Diabetes
  • Exendin(9-39)
  • Exendin-4
  • Glucagon-like peptide-1
  • Glucagon-like peptide-1 receptor
  • Islet imaging
  • Molecular imaging
  • β-Cell imaging
  • β-Cell mass

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology


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