Synthesis and evaluation of a glibenclamide glucose-conjugate: a potential new lead compound for substituted glibenclamide derivatives as islet imaging agents.

@article{Schneider2007SynthesisAE,
  title={Synthesis and evaluation of a glibenclamide glucose-conjugate: a potential new lead compound for substituted glibenclamide derivatives as islet imaging agents.},
  author={Stephan Schneider and Sandra Ueberberg and Anton Korobeynikov and Wolfgang Schechinger and Christina Schwanstecher and Mathias Schwanstecher and Harald H. Klein and Esther Schirrmacher},
  journal={Regulatory peptides},
  year={2007},
  volume={139 1-3},
  pages={122-7}
}
The search for novel SUR1-ligands originates from the idea to influence the in vivo behaviour by adding new structural moieties to the glibenclamide structure while preserving its binding affinity. Important application of novel conjugates might be their use as radioactively labelled tracer probes in the non-invasive investigation of the islet mass. It is known that the imaging quality of a tracer could be improved by increasing its hydrophilicity, which leads to a reduced plasma protein… CONTINUE READING

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Interestingly , in vivo the hypoglycaemic action of the conjugate was of significant shorter duration compared to glibenclamide .
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