Table 3.
Cell membrane permeability and activation constants for selected cyclic nucleotide analogs
Analog | cNMP conc. inside platelets (% of external) | cNMP conc. inside CHO cells (% of external) | Lipophilicitya log K w | Activationb PKG Iβ K a (μM) | Activationb PKA II K a (μM) |
---|---|---|---|---|---|
cGMP | 0.77 | 0.9 | |||
2′-dcGMP (17) | 0.5 ± 0.1 | 0.3 ± 0.5 | 0.66 | 21 | |
8-Br-cGMP (15) | 12.1 ± 3.5 | 13.5 ± 11.5 | 1.17 | 1.0 | |
8-pCPT-cGMP (16) | 19.6 ± 4.7 | n/d | 2.52 | 0.9 | |
8-Br-PET-cGMP (22) | 30.9 ± 5.7 | 24.1 ± 9.7 | 2.83 | 0.009 | |
cAMP | 1.09 | 0.08 | |||
2′-dcAMP (6) | 0.2 ± 0.3 | 0.1 ± 0.2 | 0.97 | n/d | |
8-Br-cAMP (4) | n/d | n/d | 1.35 | 0.09 | |
Sp-5,6-DCl-cBIMPS (11) | n/d | n/d | 2.99 | 0.12 |