Table 21.
| Compd | Peptidea | Y2 EC50 (nM) | Y2 Ki (nM) | Y1 Ki (nM) | Y5 Ki (nM) |
|---|---|---|---|---|---|
| 186 | PYY (3-36) | 0.3 | 0.4 | 21 | 20 |
| 187 | PYY (22-36) | 11 | 3 | 390 | >1000 |
| 188 | PYY (25-36) | 240 | 270 | >1000 | >1000 |
| 189 | AcPYY (22-36) | 13 | 9 | 118 | >1000 |
| 190 | AcPYY (24-36)-L31 | 6 | 5 | 210 | >1000 |
| 191 | AcPYY (25-36) | 27 | 30 | >1000 | >1000 |
| 192 |
|
3 | 4 | >1000 | >1000 |
| 193 |
|
4 | 11 | >1000 | >1000 |
| 194 |
|
6 | 7 | >1000 | >1000 |
| 195 |
|
25 | 41 | 4000 | 1600 |
| 196 |
|
6.5 | 9.1 | 760 | 630 |
| 197 | (Ahx5-24)NPYb | 9 | 5 | 100 | >1000 |
| 198 | Ac-YKK(Kp)(Ahx5-24)ANPYc | nd | 26.1 | nd | nd |
All peptides are amidated at the C-terminal. PYY(25-36)-L31 or PYY(24-36)-L31 are peptides in which Val 31 of corresponding PYY peptide is replaced with Leu.
5-24 amino acid residues of NPY are replaced with 6-aminohexanoic acid.
Kp is Nε-palmitoyl-L-lysine.
nd: not determined.