Pharmacological properties of the human ETB receptor and the ETB/EGFP fusion protein
| KiValues | ||
|---|---|---|
| ETB Receptor | ETB/EGFP Fusion Protein | |
| nM | nM | |
| ET1 | 0.059 ± 0.01 (6) | 0.046 ± 0.01 (6) |
| ET3 | 0.077 ± 0.01 (5) | 0.045 ± 0.01 (5) |
| BQ788 | 0.91 ± 0.2 (3) | 0.89 ± 0.2 (3) |
| BQ123 | >1000 (3) | >1000 (3) |
| PD145065 | 7.9 ± 0.6 (3) | 7.5 ± 0.6 (3) |
| Cy3-ET1 | 0.272 ± 0.07 (4) | 0.174 ± 0.04 (4) |
| Fluo-ET1 | 0.091 ± 0.01 (4) | 0.071 ± 0.01 (4) |
The Ki values for the unlabeled ligands were obtained in competition binding assays by displacement of 20 pM125I-ET1. The displacement experiments were performed with membrane preparations of CHO clones stably expressing either the human ETB receptor or the ETB/EGFP fusion protein. All values are mean ± S.D., performed in duplicate. In parentheses: total number of independent experiments.