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Åke Lernmark

Principal investigator

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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

Summary, in 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.

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

Topic

  • Biological Sciences

Status

Published

ISBN/ISSN/Other

  • ISSN: 1090-2104