Table 2 Binding affinities at NPY Y1- and Y2-receptors and Y1-related functional characteristics
Analog number | Binding affinitya | Functional assay | |
|---|---|---|---|
| Â | Y 1 | Y 2 | cAMP for Y 1 |
DOTA-free analogs | |||
1 | 11 ± 7 | > 1,000 | Antagonist |
3 | 9.0 ± 3 | > 1,000 | Antagonist |
5 | 143 ± 20 | > 1,000 | ND |
7 | 19 ± 5 | > 1,000 | Antagonist |
9 | 127 ± 50 | > 1,000 | Antagonist |
DOTA-coupled analogs | |||
2 | 143 ± 37 | > 1,000 | Antagonist |
4 | 294 ± 33 | > 1,000 | Antagonist |
6 | > 1000 | > 1,000 | ND |
8 | 29 ± 7 | > 1,000 | Antagonist |
10 | 283 ± 52 | > 1,000 | Antagonist |
11 | 13 ± 3 | > 1,000 | Antagonist |