Table 2.
Agonist and Antagonist Activity of EP Receptors in Human TM and SC Cells
|
PG Receptor Agonist |
Versus |
TM |
SC |
||||
|
Emax, % |
EC50/IC50, M |
Kb, nM |
Emax, % |
EC50/IC50, M |
Kb, nM |
||
| 17-phenyl PGF2α | Vehicle | 88 | 7.90E-10 | - | 81 | 1.30E-09 | - |
| EP1/3 agonist Sulprostone | Vehicle | 101 | 1.1E-06 | - | 86 | 3.6E-07 | - |
| 0.5 μM SC-51322 | 137 | 1.8E-06 | 770 | 139 | 1.1E-06 | 244 | |
| vs. | 0.5 μM compound 3ap | 86 | 8.8E-07 | NA | 135 | 1.6E-06 | 148 |
| 0.5 μM (SC51322+3ap) | 105 | 2.6E-06 | 377 | 104 | 1.5E-06 | 154 | |
| EP2 agonist Butaprost | Vehicle | 77 | 5.6E-07 | - | 47 | 1.7E-07 | - |
| PF-04418948 | 106 | 1.4E-06 | 674 | 44 | 5.9E-07 | 420 | |
| EP4 agonist L-902688 | Vehicle | 14 | 3.4E-08 | - | 23 | 6.9E-08 | - |
| 0.3 μM GW-627368 | 17 | 1.0E-07 | 148 | 20 | 3.2E-06 | 7 | |
NA, no antagonism. E max is relative to 10−6 M 17-phenyl PGF2α.. EC50, IC50, and Kb are described in the Cell Impedance Assay of the Methods section. Data shown as mean of n = 3 cell strains for each cell type.