Receptor activation by triptorelin in the presence or absence of different concentrations of HMA or FD-1
Ca2+ -mediated luciferase activity in CHO cells that stably express the human gonadotropin-releasing hormone receptor and NFAT-luciferase reporter gene. Values are means (± S.E.M.) of at least three separate assays performed in duplicate.
Compound | Activity in Luciferase Assay | ||
|---|---|---|---|
| EC50 | Emax | ||
| nM | % | ||
| Triptorelin | 0.24 ± 0.02 | 100 ± 2 | |
| + 3 μM HMA | 0.21 ± 0.03 | 95 ± 5 | |
| + 5 μM HMA | 0.24 ± 0.03 | 89 ± 3*** | |
| + 10 μM HMA | 0.29 ± 0.02* | 58 ± 1*** | |
| + 0.3 μM FD-1 | 2.7 ± 0.04*** | 93 ± 1*** | |
| + 1 μM FD-1 | 10 ± 2*** | 84 ± 5*** | |
| + 3 μM FD-1 | 44 ± 12*** | 72 ± 5*** | |