Inhibitory activities of YM976 and other compounds on PDE4 subtypes and [3H]rolipram binding
| IC50 | ||||
|---|---|---|---|---|
| YM976 | Rolipram | RP73401 | CDP840 | |
| nM | ||||
| [3H]Rolipram | 2.6 ± 0.18 | 1.2 ± 0.092 | 0.40 ± 0.081 | 15 ± 1.4 |
| PDE4A | 3.5 ± 0.48 | 690 ± 84 | 0.90 ± 0.11 | 27 ± 3.9 |
| PDE4B | 1.0 ± 0.065 | 270 ± 67 | 0.32 ± 0.079 | 10 ± 3.6 |
| PDE4C | 13 ± 1.9 | 1900 ± 150 | 4.8 ± 0.57 | 63 ± 19 |
| PDE4D | 1.7 ± 0.46 | 260 ± 32 | 0.42 ± 0.062 | 14 ± 3.6 |
Displacement of [3H]rolipram binding was examined using rat brain membranes. Inhibitory activities against PDE4 subtypes were evaluated with cloned human proteins of each PDE4 subtype. Data are expressed as means with 95% confidence limit of three to eight experiments. Used isoforms of PDE4A, PDE4B, PDE4C, and PDE4D were PDE4A4B, PDE4B1A, PDE4C1B, and PDE4D3A, respectively.