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

Abstract：

: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 beta-cells. To evaluate in vitro receptor specificity, binding assay was performed using dispersed mouse islet cells. Binding assay showed competitive inhibition of [(125)I]BH-exendin(9-39) binding by non-radioactive exendin(9-39). To assess in vivo selectivity, the biodistribution was evaluated by intravenous administration of [(125)I]BH-exendin(9-39) to mice. Radioactivity of harvested pancreas reached highest levels at 60 and 120min among organs examined except lung. Pre-administration of excess non-radioactive exendin(9-39) remarkably and specifically blocked the radioactivity of pancreas. After [(125)I]BH-exendin(9-39) injection into transgenic mice with pancreatic beta-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 beta-cell imaging.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Mukai E,Toyoda K,Kimura H,Kawashima H,Fujimoto H,Ueda M,Temma T,Hirao K,Nagakawa K,Saji H,Inagaki N

doi

10.1016/j.bbrc.2009.09.014

subject

Has Abstract

pub_date

2009-11-20 00:00:00

pages

523-6

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(09)01792-6

journal_volume

389

pub_type

杂志文章

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