EC50 values of inverse agonists on the inhibition of basal IPs
| Ligand | EC50 | |
|---|---|---|
| A271E | A293E | |
| nM | ||
| Indoramin | 5.48 | 187 |
| Prazosin | 1.20 | 1.09 |
| Terazosin | 12.0 | 8.90 |
| WB 4101 | 7.12 | 38.3 |
| Tamsulosin | N.D. | 2.03 |
| Phentolamine | 4.68 | 47.5 |
| Spiperone | 57.7 | 79.9 |
Concentration-dependent inhibition of basal IP accumulation was measured in COS-7 cells expressing the constitutively active A271E and A293E mutants. Values are means of two to six independent determinations done in triplicate that did not differ by >40%.
N.D., not determined.