Table 1.
Potency of prostanoid and EP/IP-selective agonists at suppressing GM-CSF generation
| Prostanoid | n | Receptor selectivitya | Inhibition of GM-CSF release pIC50 | e.c.r. PGE2=1 |
|---|---|---|---|---|
| PGE2 | 13 | EP1≈EP2 ≈EP3≈EP4 | 8.61±0.43 (78.6±6.2) | 1 |
| ONO-AE1-259 | 8 | EP2>>>EP1=EP3=EP4 | 8.79±0.26 (8.79±0.3) | 0.7 |
| 16,16-dimethyl PGE2 | 7 | EP2⩾EP3=EP1>EP4 | 7.13±0.37 (83.0±9.2) | 30 |
| Misoprostol | 5 | EP2=EP3>EP1>EP4 | 5.64±0.25 (64.7±6.9) | 935 |
| Butaprost | 4 | EP2>>EP1>EP3>EP4 | 5.43±0.26 (56.1±10.9) | 1518 |
| Cicaprostb | 11 | IP>EP4 | 9.45±0.26 | 0.14 |
| >5 | >4081 | |||
| PGF2α | 4 | FP | >5 (12.5±17.9%) | >4081 |
| PGD2 | 4 | DP | >5 (13.4±13.6%) | >4081 |
| U-46619 | 9 | TP | >5 (−22.1±11.2%) | >4081 |
| 17-phenyl-ω-trinor PGE2 | 4 | EP1>EP3>EP2>EP4 | >5 (9.7±11.8%) | >4081 |
| Sulprostone | 4 | EP3>EP1>>EP2>EP4 | >5 (−22.7±8.6%) | >4081 |
Values in parentheses show the percentage inhibition of GM-CSF release evoked by 10 μM prostanoid agonist. Equieffective concentration ratios >1 and <1 indicate that the agonist in question is less and more potent than PGE2, respectively.
a
Selectivity derived from studies in isolated cells and tissues.
b
Concentration–response curve described by a two site sigmoidal function.