Potencies of NPY, PP, and NPY analogs for the cloned human or rat NPY receptor subtypes.
| Peptide | Ki | |||
|---|---|---|---|---|
| Y1 | Y2 | Y4 | Y5 | |
| nM | ||||
| NPY | 0.6 ± 0.1 | 2.2 ± 0.2 | N.D. | 2.5 ± 0.4 |
| PP | N.D. | N.D. | 0.04 ± 0.009 | N.D. |
| 1[d-Arg25]-NPY | 0.2 ± 0.02 | 28.1 ± 5.0 | 577 ± 83 | 118.2 ± 22 |
| 2[d-His26]-NPY | 0.5 ± 0.04 | 44.4 ± 6.4 | 1,669 ± 268 | 188 ± 58.4 |
| 3[d-Arg25,d-His26]-NPY | 13.6 ± 1.7 | 642 ± 208 | 10,632 ± 3,620 | 9,279 ± 1,440 |
| 4Des-AA10-17 [Cys7,21, Pro34]-NPY | 0.3 ± 0.03 | 345 ± 237 | 5.0 ± 1.8 | 169 ± 21.9 |
| 5 Des-AA11-18 [Cys7,21,d-Lys9 (Ac)]-NPY | 0.5 ± 0.05 | 3.2 ± 0.42-a | 143 ± 472-a | 213 ± 20.8 |
| 6 Des-AA11-18 [Cys7,21,d-Lys9 (Ac), Pro34]-NPY | 0.4 ± 0.16 | 270 ± 28.4 | 3.2 ± 0.34 | 348 ± 74.1 |
| 7 Des-AA11-18 [Cys7,21,d-Lys9 (Ac),d-His26]-NPY | 5.3 ± 1.32 | 509 ± 239 | >20,000 | >20,000 |
| 8 Des-AA11-18 [Cys7,21,d-Lys9 (Ac), d-His26, Pro34]-NPY | 5.1 ± 0.97 | >20,000 | 74.2 ± 18.6 | >20,000 |
The ability of NPY, PP, and various NPY analogs to inhibit forskolin-stimulated cAMP production in HEK 293 or CHO-K1 cells expressing one of the four human or rat NPY receptor subtypes was measured. cAMP assays were done in triplicate. The values are the mean ± S.E.M. of three determinations except where noted.
N.D., not determined.
↵2-a Mean ± S.D. (n = 2).