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Table 3 Potency and intrinsic activity of all ligands for cAMP accumulation and inhibition of proliferation assays, in HLF

From: The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response

Agonist cAMP Proliferation vs serum Proliferation vs PDGF
pEC50 Emax (% max) pEC50 Emax (% max) pEC50 Emax (% max)
Treprostinil 6.82 ± 0.06 101 ± 0.58 6.99 ± 0.27 42.5 ± 5.36 7.53 ± 0.12 63.7 ± 6.39
MRE-269 6.75 ± 0.15 52.9 ± 4.36 NC NC 6.50 ± 0.23 85.7 ± 7.65
Iloprost 7.11 ± 0.34 99.5 ± 7.22 NC NC NC NC
BMY-45778 7.25 ± 0.09 50.0 ± 4.59 ND ND ND ND
Beraprost 6.98 ± 0.08 107 ± 8.99 ND ND ND ND
PGE2 7.34 ± 0.10 85.5 ± 8.64 7.04 ± 0.18 43.1 ± 6.14 8.60 ± 0.08 71.0 ± 3.86
Misoprostol 6.97 ± 0.06 52.4 ± 6.23 6.74 ± 0.10 34.7 ± 0.71 6.13 ± 0.04 94.1 ± 1.59
Butaprost 5.81 ± 0.16 8.76 ± 3.25 7.19 ± 0.38 29.1 ± 7.29 NC NC
AGN-205204 6.62 ± 0.12 49.7 ± 3.84 6.91 ± 0.48 51.3 ± 8.89 7.45 ± 0.25 101 ± 3.71
Formoterol 9.38 ± 0.20 103 ± 4.60 9.58 ± 0.29 37.2 ± 2.64 9.08 ± 0.72 70.1 ± 2.96
Indacaterol 8.58 ± 0.20 83.3 ± 4.47 7.96 ± 0.35 47.9 ± 1.58 8.84 ± 0.28 90.3 ± 5.25
Salbutamol 7.36 ± 0.34 68.9 ± 1.40 7.04 ± 0.57 32.4 ± 5.84 7.98 ± 0.17 69.2 ± 5.53
Salmeterol 9.91 ± 0.16 45.8 ± 3.53 9.58 ± 0.14 37.7 ± 7.33 10.5 ± 0.15 89.2 ± 0.27
α-MSH NC NC NC NC NC NC
NECA 5.39 ± 0.13 47.3 ± 3.40 NC NC 6.94 ± 0.43 37.8 ± 14.7
CGS-21680 NC NC NC NC NC NC
BAY60–6583 6.57 ± 0.06 10.2 ± 2.89 5.30 ± 0.16 100 ± 0.01 5.30 ± 0.12 100 ± 0.01
Dopamine 5.39 ± 0.07 41.2 ± 10.0 ND ND 4.78 ± 0.27 73.5 ± 13.5
Forskolin NC NC 5.28 ± 0.13 74.0 ± 6.70 5.98 ± 0.14 90.8 ± 9.12
IBMX NC NC NC NC NC NC
Rolipram NC NC NC NC NC NC
  1. Potency and intrinsic activity values for a range of Gs-coupled receptor agonists, PDE inhibitors, and forskolin in cAMP accumulation and BrdU inhibition assays in HLF. For cAMP accumulation intrinsic activity was calculated as a percentage of the maximal forskolin response. For BrdU inhibition intrinsic activity was calculated as a percentage of maximal proliferation observed with serum or PDGF, as indicated. Data were expressed as means ± SEM for at least 3 independent experiments
  2. NC not calculated due to incomplete curve, ND not determined in this assay