Affinities of NPY, PP and NPY analogs for the cloned human NPY Y1, Y2, Y4, and Y5 receptor subtypes.
| Peptide | Ki | |||
|---|---|---|---|---|
| Y1 | Y2 | Y4 | Y5 | |
| nM | ||||
| NPY | 0.28 ± 0.06 | 1.2 ± 0.3 | N.D. | 1.5 ± 0.1 |
| PP | N.D. | N.D. | 0.07 ± 0.03 | N.D. |
| 1[d-Arg25]-NPY | 0.9 ± 0.2 | 11.6 ± 2.9 | 74.6 ± 21.3 | 43.4 ± 4.2 |
| 2[d-His26]-NPY | 2.0 ± 0.3 | 29.0 ± 4.7 | 20.1 ± 1.9 | 34.6 ± 3.8 |
| 3[d-Arg25,d-His26]-NPY | 9.7 ± 0.6 | 399 ± 35.5 | 852 ± 114 | 3003 ± 440 |
| 4Des-AA10-17 [Cys7,21, Pro34]-NPY | 0.2 ± 0.05 | 37.0 ± 12.4 | 5.0 ± 1.8 | 22.6 ± 5.0 |
| 5 Des-AA11-18 [Cys7,21,d-Lys9 (Ac)]-NPY | 0.7 ± 0.1 | 1.4 ± 0.1 | 53.5 ± 7.9 | 77.1 ± 36.1 |
| 6Des-AA11-18 [Cys7,21, d-Lys9 (Ac), Pro34]-NPY | 0.2 ± 0.01 | 124 ± 11.3 | 7.3 ± 1.1 | 55.9 ± 7.4 |
| 7 Des-AA11-18[Cys7,21, d-Lys9 (Ac),d-His26]-NPY | 2.2 ± 0.3 | 1.4 ± 0.3 | 206 ± 16.8 | 3023 ± 164 |
| 8Des-AA11-18 [Cys7,21, d-Lys9 (Ac),d-His26, Pro34]-NPY | 1.2 ± 0.1 | 801 ± 41.4 | 31.4 ± 1.3 | 2363 ± 142 |
Competition binding assays were performed using membranes prepared from CHO-K1 cells expressing one of the human NPY receptor subtypes. Binding assays were performed in duplicate. Each value is the mean ± S.E.M. of three to four determinations.
N.D., not determined.