| Receptor Binding Activity | Adenylyl Cyclase |
---|
Glucagon and Analogues | Relative Affinitya, (%) | Fold Decrease | Relative Potencyb, (%) | Maximum Activityc (%) | pA2d Value |
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1A Glucagon | 100 | | 100 | 100 | — |
1B Glucagon amide | 100 | | 15 | 100 | — |
1C DesHis1glucagon | 8 | 12.5 | 0.1 | 36 | — |
1D DesHis1glucagon amide | 63 | 1.6 | 0.16 | 44 | — |
2 Cyclic[Glu2Lys5]-amide | 0.41 | 244 | 0.58 | 100 | |
3 Cyclic[Glu9Lys12]-amide | 4.8 | 21 | 0.126 | 18 | — |
4 DesHis1cyclic[Glu9 Lys12]-amide | 12.6 | 8 | <0.00013 | — | 6.9 |
5 DesHis1Glu9cyclic[Glu20 Lys24]-amide | 19.1 | 5.3 | <0.003 | — | 6.8 |
- aThe ratio of unlabeled glucagon concentration required to displace 50% of receptor-bound [125I]-glucagon, IC50, to the concentration required for analogues of glucagon × 100.
- bThe ratio of glucagon concentration at 50% stimulation (EC50) of natural glucagon to that of glucagon analogue × 100.
- cThe ratio of maximum response of glucagon analogue to that of natural glucagon × 100.
- dpA2 value is the negative logarithm of the concentration of inhibitor that reduces the response to 1 unit of agonist to the response obtained from 0.5 unit of agonist.