Binding inhibitory potency (Ki) and Hill coefficient of tezosentan on the two ET receptor subtypes
| Receptor Subtype | Cell or Tissue | Membranes or Whole Cells | Radioactive Ligand | n | Ki | Hill CoefficientnH |
|---|---|---|---|---|---|---|
| nM | ||||||
| ETA | Sf9 | M | ET-1 | 6 | 18 ± 4 | 1.04 ± 0.07 |
| CHO | C | ET-1 | 3 | 0.3 ± 0.2 | 0.83 ± 0.08 | |
| ETB | Human placenta | M | ET-1 | 5 | 21 ± 3 | 0.83 ± 0.06 |
| Porcine trachea | M | S6c | 5 | 10 ± 2 | 0.62 ± 0.06 | |
| Rat EC | C | ET-3 | 4 | 11 ± 4 | 0.71 ± 0.05 |
Binding was performed either on whole cells in culture (C) or on membrane preparations from cells or tissues (M); n, number of experiments. Sf9, baculovirus-infected insect cells expressing human ETA receptors; CHO, Chinese hamster ovary cells expressing human ETA receptors; EC, endothelial cells; S6c, sarafotoxin S6c.