Table 3.
Agonist relative potencies in PSV in the absence of the EP4 receptor antagonist GW627368X (10 μM) together with comparative data generated at human recombinant EP4 receptors expressed in HEK 293 (T) cells (Wilson et al., 2004)
| Agonist | PSV | HEK hEP4 |
|---|---|---|
| PGE2 | 1 | 1 |
| PGE1 | 1 | 2 |
| 11-deoxy-PGE1 | 13 | 3 |
| 16,16-dimethyl-PGE2 | 30 | 40 |
| 17-phenyl-ω-trinor PGE2 | 320 | 120 |
| BW245C | 80 | 200 |
| PGF2α | 1000 | 5000 |
| Iloprost | 500 | 10,000 |
| GR63799X | 790 | 200 |
| Misoprostol | 250 | 400 |
| Cicaprost | 630 | 790 |
| PGI2 | 1260 | 2500 |
| 19-(R)-hydroxy-PGE2 | 250 | 3200 |
| PGD2 | 500 | 6300 |
| Sulprostone | 790 | 32,000 |
| Cloprostenol | 2000 | >63,000 |
| Fluprostenol | >63,000 | |
| Butaprost FA | 1260 | >200,000 |
| Butaprost ME | 790 | >2,000,000 |
A subset of compounds (indicated in italics) were shifted by >3-fold by 10 μM GW627368X and are therefore assumed to be acting predominantly through EP4 receptors.