Table 3. Affinities of the agonists for the binding site of the receptor labelled by [3H]SQ29,548 in HEK293 cells transiently expressing the WT or the mutant human TP receptors.
Agonist | WT Ki, nM±%CV | E129V Ki, nM±%CV | Affinity ratioa |
U46619 | 169.90±13 | 16.32±18** | 10.4 |
I-BOP | 24.27±18 | 3.90±21** | 6.2 |
8-isoPGE2 | 2916±15 | 547.6±2** | 5.3 |
8-isoPGF2α | 12930±19 | 2908±11** | 4.4 |
Ki values were obtained by simultaneous analysis of at least 3 independent competition experiments analyzed with GraphPad Prism implemented with the LIGAND model (see Data and statistical analysis).
Affinity ratio was calculated as the ratio of the Ki for the WT TP receptor over the Ki of the E129V mutant.
p<0.01 vs. WT.