Table 1.
Inhibitor studies of PDE11A2 and PDE11A3 expressed in Sf-9 cells
| Inhibitor | PDE Selectivity (IC50) | IC50 (n = 3) for PDE 11A2 | IC50 (n = 3) for PDE 11A3 |
|---|---|---|---|
| IBMX | Nonselective (2–50 μM) | 80 ± 43 μM | 25 ± 10 μM |
| Papaverine | Nonselective (5–25 μM) | >100 μM | ND |
| EHNA | PDE 2 (1.0 μM) | >100 μM | ND |
| Rolipram | PDE 4 (2.0 μM) | >200 μM | ND |
| Dipyridamole | PDE 5 (0.9 μM) | 1.8 ± 1.1 μM | 0.82 ± 0.1 μM |
| PDE 6 (0.38 μM) | |||
| PDE 7 (9.0 μM) | |||
| PDE 8 (4.5 μM) | |||
| PDE 10 (1.1 μM) | |||
| SCH 51866 | PDE 1 & 5 (0.1 μM) | >100 μM | ND |
| PDE 7 (35 μM) | |||
| PDE 9 (1.5 μM) | |||
| PDE 10 (1.0 μM) | |||
| Enoximone | PDE 3 (1.0 μM) | >100 μM | ND |
| Sildenafil | PDE 5 (3.9 nM) | >500 nM | ND |
| Ro 201724 | PDE 4 (2.0 μM) | >200 μM | ND |
| Zaprinast | PDE 5 (0.76 μM) | 28 ± 7.6 μM | 5.0 ± 1.4 μM |
| PDE 6 (0.15 μM) | |||
| Pentoxifylline | Nonselective (45–150 μM) | >100 μM | ND |
ND, not determined. Conditions for inhibitor studies are described in Materials and Methods.