Potencies and efficacies of CCK-9 and modified peptides to stimulate inositol phosphates production on the WT-CCK2R, N358A (N6.55A), and Tyr189F (Y4.60F) mutant
| CCK-9 | (PheCH3)9-CCK | (Phenylethylamide)9-CCK | ||||
|---|---|---|---|---|---|---|
| EC50 | Emax | EC50 | Emax | EC50 | Emax | |
| nM | % | nM | % | nM | % | |
| WT-CCK2R | 0.69 ± 0.97 | 100 | 11.2 ± 2.9 | 85 | 111 ± 22 | 40 |
| N358A mutant | 20.9 ± 7.4 | 90 | 38.2 ± 7.5 | 70 | 450 ± 73 | 41 |
| Y189F mutant | 41.9 ± 6.3 | 90 | 320 ± 33 | 48 | N.A. | 20 |
Potencies (EC50) of the indicated ligands were calculated from total IP production dose-response curves. Results are expressed as mean ± S.E. of three to five separate experiments performed in duplicate. The efficacies (Emax) of the peptides tested to stimulate IP production are expressed as the percentage of the maximal increase obtained using 10−6 M CCK-9 on the WT-CCK2R.
N.A., not applicable.