Ability of various ligands to inhibit binding of 125I-BH-CCK-8 in COS-7 cells transiently expressing the rat or mouse CCK-AR
| Ligand | Mouse CCKAR Ki | Rat CCKARKi |
|---|---|---|
| nM | ||
| CCK-8 | 1 ± 0.3 | 1 ± 0.3 |
| JMV-180 | 30 ± 2.5 | 20 ± 2.5 |
| SR-49,344 | 25 ± 2 | 20 ± 2.5 |
| L-364,718 | 25 ± 2.5 | 12.5 ± 2.5 |
| JMV-379 | 35 ± 2.5 | 35 ± 2.5 |
| PD-170,292 | 35 ± 2.5 | 25 ± 2.5 |
| L-365,260 | nd | nd |
| PD-135,158 | nd | nd |
The IC50 values were determined as indicated underExperimental Procedures and in the text. Each value represents the mean ± S.D. of at least three separate experiments performed in triplicate. For each experiment, the nonspecific binding was approximately 5 to 10% of the total binding.
nd, no displacement.