• Potent and specific inhibitor of cGMP-specific phosphodiesterase with IC50 = 230 nM. It levates the intracellular cGMP level without causing any change in the cAMP level in isolated porcine coronary arteries and it has no effect on other PDE isozymes
OTAVAchemicals Catalogue Number: 7020540496
CAS Registry Number: 150450-42-3
Purity: 95%+ (HPLC)
Ref.: Takase et al. Cyclic GMP Phosphodiesterase Inhibitors. 2. Requirement of 6-Substitution of Quinazoline Derivatives for Potent and Selective Inhibitory Activity. Journal of Medicinal Chemistry (1994), 37, 2106-2111
Abstract: 4-[3,4-Methylenedioxybenzylamino]quinazolines were prepared and evaluated their inhibitory activities toward cyclic GMP phosphodiesterase (cGMP-PDE) from porcine aorta. Monosubstitution at the 6-position was essential for inhibitory activity, and the preferred substituents were compact and hydrophobic, i.e. I (R and IC50 given: OMe 0.23, Me 0.10, Cl 0.019, SMe 0.031, CN 0.090). I lacked inhibitory activity toward other phosphodiesterase isoenzymes (all IC50 values > 100 μM), and their relaxing activities in porcine coronary arteries were well correlated with the inhibitory activities toward cGMP-PDE (r = 0.88, p < 0.05). I (R = OMe) elevated the intracellular cGMP level in isolated porcine coronary arteries without causing any change in the cAMP level. This series of compounds dilates coronary arteries via potent and specific inhibition of cGMP-PDE.