Table 1 Basic characteristics of PDE3, PDE4, PDE5, and their selective chemical inhibitors.
PDE isoform | cGMP Km (μmol/L) | cAMP Km (μmol/L) | Tissue distribution | Inhibitors | IC50 | Ref |
|---|---|---|---|---|---|---|
PDE3A | 0.02–0.15 | 0.18 | Heart; vascular smooth muscle; platelets; oocyte; kidney | Milrinone | 150 nmol/L | |
PDE3B | 0.28 | 0.38 | Vascular smooth muscle; adipocytes; hepatocytes; kidney; β cells; developing sperm; T lymphocytes; macrophages | Amrinone | 16.7 μmol/L |  |
|  |  |  |  | Enoximone | 1.8 μmol/L |  |
|  |  |  |  | Pimobendan | 2.4 μmol/L |  |
| Â | Â | Â | Â | Cilastazol | 200 nmol/L | Â |
PDE4A | – | 2.9–10 | Ubiquitous | Rolipram | 1 μmol/L | |
PDE4B | – | 1.5–4.7 | Ubiquitous | Ro 20-1724 | 2 μmol/L |  |
PDE4C | – | 1.7 | Lung; testis; neuronal cells | Cilomilast | 120 nmol/L |  |
PDE4D | – | 1.2–5.9 | Ubiquitous | Roflumilast | 0.8 nmol/L |  |
PDE5A | 2.9–6.2 | 290 | Platelets; vascular smooth muscle; brain; lung; heart; kidney; skeletal muscle | Sildenafil | 4 nmol/L | |
| Â | Â | Â | Â | Vardenafil | 0.1 nmol/L | Â |
| Â | Â | Â | Â | Tadalafil | 2 nmol/L | Â |
| Â | Â | Â | Â | Udenafil | 6 nmol/L | Â |