Compound | IC50 Values ± S.E.M. (nM) for Several Assays | |||||
---|---|---|---|---|---|---|
PDE4AQT | PDE4BQT | PDE4CQT | PDE4DQT | HWBA (TNF-α) | HMCA (TNF-α) | |
L-826,141 | 1.26 ± 0.15 (9)a | 0.38 ± 0.07 (5) | 2.38 ± 0.8 (5) | 0.26 ± 0.04 (5) | 310 ± 48 (21) | 31 ± 13 (6) |
R-rolipram | 4.8 ± 1.3 (9) | 5.4 ± 2.0 (6) | 40.5 ± 7 (8) | 3.9 ± 1.0 (8) | 2156 ± 204 (15) | 288 ± 125 (8) |
Roflumilast | 0.16 ± 0.03 (3) | 0.11 ± 0.01 (4) | 0.61 ± 0.05 (4) | 0.11 ± 0.01 (4) | 140 ± 23 (15) | 1.29 ± 0.55 (5) |
Roflumilast N-oxide | 0.58 ± 0.03 (4) | 0.37 ± 0.05 (4) | 3.2 ± 0.5 (4) | 0.31 ± 0.04 (4) | 200 ± 65 (20) | 1.63 ± 0.65 (4) |
HWBA, human whole blood assay; HMCA, human mononuclear cell assay.
↵ a n, number.