Relative potencies and functional activity of IP receptor agonists in BEAS-2B cells
| Functional Output | ||||||||
|---|---|---|---|---|---|---|---|---|
| Inhibition of CXCL9 Release | Inhibition of CXCL10 Release | Induction of CRE-Reporter | Augmentation of GRE-Reporter | |||||
| p[A]50 | Max | p[A]50 | Max | p[A]50 | Max | p[A]50 | Δa | |
| % | % | fold | fold | |||||
| Iloprost | −9.08 ± 0.07 (6)b | 20.9 ± 2.6 (6)b | −8.93 ± 0.06 (7)b | 24.7 ± 2.5 (6)b | −8.12 ± 0.04 (6) | 3.60 ± 0.22 (6) | −8.00 ± 0.04 (3) | 26.1 ± 1.3 (3) |
| Iloprost + Antagonistsc | Inactive at 1 μM | Inactive at 1 μM | −8.09 ± 0.04 (6) | 3.80 ± 0.23 (6) | −8.01 ± 0.04 (3) | 26.8 ± 1.4 (3) | ||
| Taprostene | −7.30 ± 0.05 (7) | 35.5 ± 1.8 (7) | −7.26 ± 0.07 (7) | 35.7 ± 1.9 (7) | −7.19 ± 0.06 (6) | 3.55 ± 0.10 (6) | −6.53 ± 0.21 (3) | 34.3 ± 2.1 (3) |
| Taprostene + Antagonistsc | −7.40 ± 0.17 (7) | 33.4 ± 1.6 (7) | −7.26 ± 0.11 (7) | 33.4 ± 2.5 (7) | −7.18 ± 0.05 (6) | 3.52 ± 0.18 (6) | −6.63 ± 0.05 (3) | 35.3 ± 2.0 (3) |
| 15-Deoxy-TIC | −7.76 ± 0.03 (3) | 43.1 ± 1.7 (3) | −7.79 ± 0.01 (3) | 42.3 ± 0.5 (3) | Inactive at 1 μM | Inactive at 1 μM | ||
| 15-Deoxy-TIC + Antagonistsc | −7.70 ± 0.09 (3) | 45.4 ± 1.8 (3) | −7.81 ± 0.04 (3) | 42.0 ± 0.4 (3) | Inactive at 1 μM | Inactive at 1 μM | ||
| PGI2 | −5.96 ± 0.07 (3) | 49.1 ± 1.2 (3) | −5.99 ± 0.08 (3) | 53.0 ± 1.7 (3) | —d | 6.3 ± 0.1 (4)e | —d | 8.0 ± 1.0 (3)e |
| PGI2 + Antagonistsc | −5.93 ± 0.09 (3) | 48.7 ± 1.9 (3) | −5.97 ± 0.09 (3) | 52.4 ± 2.5 (3) | —d | 6.0 ± 0.2 (4)e | —d | 7.6 ± 0.9 (3)e |
↵a Fold induction: (dexamethasone + agonist) − dexamethasone alone.
↵b Response biphasic; p[A]50 and Max values refer to high-potency component.
↵c Experiment performed in cells pretreated with BWA 868C (1 μM), L-798,106 (100 nM), and L-161,982 (500 nM).
↵d p[A]50 value could not be determined because maximum response was not attained.
↵e fold/Δ fold induction at 100 μM.