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Table 1 Pharmacological parameters of cyclic analogues of glucagon

From: The Role of Salt Bridge Formation in Glucagon: An Experimental and Theoretical Study of Glucagon Analogs and Peptide Fragments of Glucagon

  Receptor Binding Activity Adenylyl Cyclase
Glucagon and Analogues Relative Affinitya, (%) Fold Decrease Relative Potencyb, (%) Maximum Activityc (%) pA2d Value
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
  1. 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.
  2. bThe ratio of glucagon concentration at 50% stimulation (EC50) of natural glucagon to that of glucagon analogue × 100.
  3. cThe ratio of maximum response of glucagon analogue to that of natural glucagon × 100.
  4. 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.