TABLE 1

GLP-1 Receptor IC50 Values for Different GLP-1 Receptor Agonists and Antagonists

CompoundLigand/metal complexHuman insulinoma (nM)Rat insulinoma (nM)
GLP-1(7-36) controlLigand1.1 ± 0.30.8 ± 0.1
Ex(9-39)NH2Ligand10.9 ± 1.13.9 ± 1.7
[Nle14,Lys40(Ahx-DOTA)NH2]Ex-4Ligand0.9 ± 0.30.5 ± 0.2
[Lys40(Ahx-DOTA)NH2]-Ex(9-39)Ligand44.1 ± 7.08.5 ± 3.0
[Lys27(Ahx-DOTA)]-Ex(9-39)NH2Ligand48.1 ± 5.1122.3 ± 12.1
natGa137.2 ± 10.3213.2 ± 21.3
[Lys40(NODAGA)NH2]Ex(9-39)Ligand29.7 ± 10.716.3 ± 3.6
natGa46.7 ± 16.322.0 ± 5.3
[Lys27(NODAGA)]-Ex(9-39)NH2Ligand143.3 ± 56.681.0 ± 8.9
natGa71.3 ± 26.546.7 ± 9.3