Main pharmacological characteristics of the xanthines investigated in this quantitative synthesis

Adenosine receptors (antagonism, affinity)PDE (inhibitory potency)PI3 kinase (inhibitory potency)HDAC (inhibitory potency)
BamiphyllineA1/A2 562-foldNANANA
DoxofyllineA1, A2A, A2B and A3 >100 µMPDE2A 100 µM
other PDEs >100 µM (modest effect)
NAHDAC1-11 no effect
EnprophyllineA1 42–156 µM
A2A 38–81 µM
A2B 5–20 µM
A3 65–93 µM
PDE1-5 >100 µM (modest effect)NANA
Theophylline and aminophylline (theophylline ethylenediamine)A1 10–30 µM
A2A 2–10 µM
A2B 10–30 µM
A3 20–100 µM
PDE3 98 µM
PDE4 150 µM
100 µMHDAC1-11 no effect

PDE: phosphodiesterase; PI3: phosphoinositide-3; HDAC: histone deacetylase; NA: not available.