TABLE 3.
Biological activity of CCK1 receptor-based chimeric constructs expressed in CHO cells
| CCK1R-based chimeric receptors | Receptor abbreviations | GI181771X EC50 (nM) | GI181771X ratio EC50/Ki |
|---|---|---|---|
| nm | |||
| CCK1R WT | CCK1R | 6.1 ± 1.4 | 0.06 |
| N2.61T | CCK1R TM2 | 4.5 ± 1.0 | 0.05 |
| T3.28V, T3.29S | CCK1R TM3 | 2.5 ± 1.3 | 0.40 |
| I6.51V, F6.52Y | CCK1R TM6 | 19.6 ± 5.5 | 0.27 |
| L7.39H | CCK1R TM7 | NRa | |
| N2.61T, T3.28V, T3.29S | CCK1R TM (2,3) | 0.2 ± 0.1b | 0.03 |
| N2.61T, I6.51V, F6.52Y | CCK1R TM (2,6) | 5.9 ± 0.7 | 0.30 |
| N2.61T, L7.39H | CCK1R TM (2,7) | NR | |
| T3.28V, T3.29S, I6.51V, F6.52Y | CCK1R TM (3,6) | 1.4 ± 0.3b | 0.30 |
| T3.28V, T3.29S, L7.39H | CCK1R TM (3,7) | NR | |
| I6.51V, F6.52Y, L7.39H | CCK1R TM (6,7) | NR | |
| N2.61T, T3.28V, T3.29S, I6.51V, F6.52Y | CCK1R TM (2,3,6) | 0.1 ± 0.1b | 0.07 |
| N2.61T, T3.28V, T3.29S, L7.39H | CCK1R TM (2,3,7) | 1.9 ± 0.4 | 1.00 |
| N2.61T, I6.51V, F6.52Y, L7.39H | CCK1R TM (2,6,7) | NR | |
| TT3.28V, T3.29S, I6.51V, F6.52Y, L7.39H | CCK1R TM (3,6,7) | NR | |
| N2.61T, T3.28V, T3.29S, I6.51V, F6.52Y, L7.39H | CCK1R TM (2,3,6,7) | NR | |
| CCK2R WT | CCK2R | NR |
a NR, no response.
b p < 0.05 compared to values for wild-type CCK1R.