CONCLUSION
We have developed two new radioligands (an agonist and an antagonist)
for the GLP-2R; both with high affinity to the human, rat and mouse
GLP-2R. With these, we show differential binding kinetics of agonist and
antagonist to the GLP-2R, and confirm GLP-2R expression at the protein
level in the GI tract’s SEMFs and in the pancreatic islet cells.
Moreover, we demonstrate cross-activity with -binding and -activity of
GLP-2 within the GLP-1R system. These observations are of importance for
tissue localization and structural characterization for not only the
GLP-2R, but also for other class B1 GPCRs.