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. 2011 Jun 29;384(2):169–176. doi: 10.1007/s00210-011-0662-6

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

All experiments were performed three times

n/d not determined

aKrass et al. (1997)

bPoppe et al. (2008)