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Systematic screening of potential beta-cell imaging agents.

Author:
  • Ian R Sweet
  • Carla J. Cook
  • Åke Lernmark
  • Carla J. Greenbaum
  • Angela R Wallen
  • Erin S. Marcum
  • Svetlana A. Stekhova
  • Kenneth A. Krohn
Publishing year: 2004
Language: English
Pages: 976-983
Publication/Series: Biochemical and Biophysical Research Communications
Volume: 314
Issue: 4
Document type: Journal article
Publisher: Elsevier

Abstract english

The beta-cell loss seen in diabetes mellitus could be monitored clinically by positron emission tomography (PET) if imaging agents were sufficiently specific for beta-cells to overcome the high ratio of non-beta-cell to beta-cell tissue in pancreas. In this report, we present a screening assay for identifying beta-cell-specific compounds that is based on the relative accumulation and retention by islet, INS-1, and exocrine (PANC-1) cells of candidate molecules. Molecules thought to have a high affinity for beta-cells were tested and included glibenclamide, tolbutamide, serotonin, L-DOPA, dopamine, nicotinamide, fluorodeoxyglucose, and fluorodithizone. Glibenclamide and fluorodithizone were the most specific, but the specificity ratios fell well below those needed to attain robust signal to background ratio as a PET imaging agent for quantifying beta-cell mass. In vivo tests of the biodistribution of glibenclamide and fluorodithizone in rats indicated that the compounds were not specifically associated with pancreas, bearing out the predictions of the in vitro screen.

Keywords

  • Biological Sciences

Other

Published
  • ISSN: 1090-2104
E-mail: ake [dot] lernmark [at] med [dot] lu [dot] se

Principal investigator

Diabetes and Celiac Unit

+46 40 39 19 01

+46 70 616 47 79

60:11:015

Jan Waldenströms gata 35, Malmö

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Lund University Diabetes Centre, CRC, SUS Malmö, Jan Waldenströms gata 35, House 91:12. SE-214 28 Malmö. Telephone: +46 40 39 10 00