IC50 values of YM976 and related compounds on PDE activity
| Compound | IC50 | ||||
|---|---|---|---|---|---|
| PDE4 | PDE1 | PDE2 | PDE3 | PDE5 | |
| nM | μM | ||||
| YM976 | 2.2 (1.7–2.9) | >3 | >3 | >3 | >3 |
| Rolipram | 820 (540–1220) | >100 | >100 | >100 | >100 |
| RP73401 | 0.43 (0.31–0.59) | >1 | >1 | >1 | >1 |
| SB207499 | 117 (65–213) | >300 | >300 | >300 | >300 |
| CDP840 | 19 (16–23) | >30 | >30 | >30 | >30 |
Data were expressed as mean (95% confidence limits) of three to eight separate experiments. PDE4, PDE1, PDE3, and PDE5 were partially purified from human peripheral leukocytes, and PDE2 was isolated from rat ventricles.