Systematic screening of potential beta-cell imaging agents.
Sweet, Ian R ; Cook, Carla J. ; Lernmark, Åke LU
; Greenbaum, Carla J.
; Wallen, Angela R
; Marcum, Erin S.
; Stekhova, Svetlana A.
and Krohn, Kenneth A.
(2004)
In Biochemical and Biophysical Research Communications
314(4).
p.976-983
- Abstract
- 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... (More)
- 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. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1130257
- author
- Sweet, Ian R
; Cook, Carla J.
; Lernmark, Åke
LU
; Greenbaum, Carla J.
; Wallen, Angela R
; Marcum, Erin S.
; Stekhova, Svetlana A.
and Krohn, Kenneth A.
- publishing date
- 2004
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Biochemical and Biophysical Research Communications
- volume
- 314
- issue
- 4
- pages
- 976 - 983
- publisher
- Elsevier
- external identifiers
-
- scopus:0942289897
- ISSN
- 1090-2104
- DOI
- 10.1016/j.bbrc.2003.12.182
- language
- English
- LU publication?
- no
- id
- 39e1ff0f-ae6d-4ff5-b826-d67a803f9aef (old id 1130257)
- date added to LUP
- 2016-04-01 16:38:05
- date last changed
- 2022-03-15 01:50:12
@article{39e1ff0f-ae6d-4ff5-b826-d67a803f9aef,
abstract = {{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.}},
author = {{Sweet, Ian R and Cook, Carla J. and Lernmark, Åke and Greenbaum, Carla J. and Wallen, Angela R and Marcum, Erin S. and Stekhova, Svetlana A. and Krohn, Kenneth A.}},
issn = {{1090-2104}},
language = {{eng}},
number = {{4}},
pages = {{976--983}},
publisher = {{Elsevier}},
series = {{Biochemical and Biophysical Research Communications}},
title = {{Systematic screening of potential beta-cell imaging agents.}},
url = {{http://dx.doi.org/10.1016/j.bbrc.2003.12.182}},
doi = {{10.1016/j.bbrc.2003.12.182}},
volume = {{314}},
year = {{2004}},
}