Receptor affinity of FD-1 and radioligand binding capacity (in the absence of FD-1) in the presence or absence of different concentrations of HMA
Displacement of specific 125I-triptorelin binding from human gonadotropin-releasing hormone receptors stably expressed in CHO cell membranes. Values are means (±S.E.M.) of at least three separate assays performed in duplicate.
Compound | 125I-Triptorelin Displacementa | ||
|---|---|---|---|
| Ki | Bmax | ||
| nM | % | ||
| FD-1 | 4.9 ± 1 | 100 ± 5 | |
| + 3 μM HMA | 5.9 ± 2 | 87 ± 5* | |
| + 10 μM HMA | 5.3 ± 1 | 75 ± 6** | |
| + 30 μM HMA | 2.3 ± 0.7* | 47 ± 5*** | |