Table 5. cAMP Signalling Parameter Estimates of His1- and Phe1-Containing Chimeric Ligands in INS-1 832/3 Cellsa.
pEC50 (M) | Emax (%) | |
---|---|---|
GLP-1 | 8.6 ± 0.2 | 100 |
GLP-1-phe1 | 7.3 ± 0.1*,# | 100 |
Chi1 | 8.7 ± 0.2 | 100 |
Chi1-phe1 | 7.5 ± 0.1*,# | 100 |
Chi2 | 9.2 ± 0.2* | 100 |
Chi2-phe1 | 8.6 ± 0.1# | 100 |
Chi3 | 9.3 ± 0.2* | 100 |
Chi3-phe1 | 8.4 ± 0.1# | 100 |
Ex-ala2 | 9.4 ± 0.2* | 100 |
Ex-ala2-phe1 | 8.8 ± 0.1# | 100 |
Ex4 | 9.3 ± 0.2* | 100 |
Ex-phe1 | 8.4 ± 0.2# | 100 |
GLP-1-gly2 | 8.3 ± 0.1 | 100 |
GLP-1-gly2-phe1 | 6.4 ± 0.1*,# | 100 |
Mean ± SEM signaling parameter estimates from data shown in Figure 3, n = 5 experimental repeats. Signaling parameter estimates were determined from 3-parameter fitting. All compounds are full agonists for cAMP in this cell model, so Emax was globally constrained to 100%. *p < 0.05 versus GLP-1, and #p < 0.05 for Phe1 ligand versus corresponding His1 ligand, determined by one-way ANOVA with Tukey’s test.