Table II.
Properies of cyclic nucleotide analogs as PDE substrates and inhibitors by isotermal microcalorimetry. Km data for cyclic nucleotides analogs, that can be PDE substrates, are in shaded cells, while ones, that can inhibit PDEs are in non-shaded cells and presented as Ki.
| Analog | PDE1A | PDE1B | PDE1C | PDE2 | PDE4 | PDE5 | PDE6 | PDE8A | PDE9 | PDE10 |
|---|---|---|---|---|---|---|---|---|---|---|
| Km /Ki | Km /Ki | Km /Ki | Km /Ki | Km /Ki | Km /Ki | Km /Ki | Km /Ki | Km /Ki | Km /Ki | |
| cAMP | 93.1 | 33.0 | 3.19 | 112 | 5.52 | 201 | 823 | 0.63 | 230 | 0.24 |
| 8Br-cAMP | 32.8 | 63.6 | 18.0 | 38.7 | 54.4 | 23.4 | 68.8 | n.e. | 5.99 | 4.83 |
| cGMP | 8.23 | 5.35 | 4.64 | 31.0 | 24.5 | 2.01 | 10 | n.e. | 0.20 | 23.7 |
| 8-Br-cGMP | 47.2 | 4.48 | 62.8 | 90.9 | 30.1 | 79.2 | 33 | 0.55 | 0.77 | 23.7 |
| Sp-5,6-DCl-cBMPS | 89.6 | 2.25 | 55.8 | 17.7 | 18.8 | 15.1 | 24.5 | 26.7 | n.e. | 4.75 |
| 6-Bnz-cAMP | n.e. | 9.86 | 323 | 240 | 49 | 68.9 | 64.6 | n.e. | 2.27 | 45.6 |
| 8-pCPT-2-0-Me cAMP | 50.5 | 8.57 | 44.2 | 14.5 | 895 | 3.12 | 3.51 | 4.01 | n.d. | 5.84 |
| Sp-8-pCPT-2-0-Me- cAMPS | 0.38 | 2.02 | 17.2 | n.d. | 0.82 | 0.4 | 1.05 | 3.08 | n.d. | 2.42 |
| Rp-8-Br-cAMPS | n.e. | 5.57 | 37.7 | 23.3 | 28.7 | 94.7 | 106 | n.e. | n.d. | 28.1 |
| 8-pCPT-cGMP | 16.7 | 8.62 | 47.1 | 40 | 53.4 | 27.6 | 41.3 | 77.7 | 1.29 | 6.04 |
| 8-Br-Pet-cGMP | 2.4 | 2.13 | 73.1 | 98.6 | 8.84 | 5.29 | 11.2 | n.e. | n.d. | 34.4 |
| Rp-pCPT-cGMPS | 42.4 | 2.1 | 32.6 | 52.9 | 137 | 49.7 | 26 | 7.64 | n.d. | 38.6 |
| Rp-8-Br-Pet-cGMPS | n.e. | 2.5 | 55.6 | 0.76 | 8.1 | 4.09 | 13.8 | n.e. | 2.28 | 4.98 |