Table 5.
Potencies of various BODIPY®-labelled and native peptides of the NPY family in HEK293 cells transfected with either of the rat Y1, Y2, Y4 or Y5 receptor cDNA to inhibit forskolin-induced cAMP accumulation
| cAMP assay in HEK293-transfected cells (EC50) (nM) | ||||
|---|---|---|---|---|
| Peptides | Y1 | Y2 | Y4 | Y5 |
| NPY | 5±1 (3)a | 10±2 (3) | ND | 19±2 (3) |
| BODIPY®TMR-NPY | 40±5 (3)* | 65±15 (3)* | ND | 25±3 (3) |
| [Leu31, Pro34]NPY | ND | ND | ND | 30±5 (3) |
| BODIPY®TMR-[Leu31, Pro34]NPY | ND | ND | ND | 20±4 (3) |
| [Leu31, Pro34]PYY | 3.0±0.6 (3) | ND | 35±4 (3) | 15±4 (3) |
| BODIPY®-FL[Leu31, Pro34]PYY | 32±8 (3)* | ND | 80±16 (3)* | 12±3 (3) |
| PYY(3–36) | ND | 7±2 (3) | ND | 50±6 (3) |
| BODIPY®FL-PYY(3–36) | ND | 45±9 (3)* | ND | 60±8 (3) |
| hPP | ND | ND | 7±2 (3) | 9±3 (3) |
| BODIPY®FL-hPP | ND | ND | 15±3 (3) | 60±15 (3)* |
| [hPP(1–17), Ala31, Aib32]NPY | ND | ND | ND | 35±4 (3) |
| BODIPY®TMR-[hPP(1–17), Ala31, Aib32]NPY | ND | ND | ND | 40±5 (3) |
| [cPP(1–7), NPY(19–23), Ala31, Aib32, Gln34]hPP | ND | ND | ND | 22±3 (3) |
| BODIPY®TMR-[cPP(1–7), NPY(19–23), Ala31, Aib32, Gln34]hPP | ND | ND | ND | 30±5 (3) |
Data are the mean±s.e.m. of three determinations, each performed in duplicate.
a
Number in parenthesis represents the number of determinations. EC50 represents the concentration of agonist needed to inhibit 50% of cAMP accumulation induced by forskolin. ND, not determined.
*
P<0.05, fluorescent vs nonfluorescent peptide.