N-(1,3-Benzodioxol-5-ylmethyl)-6-methoxy-4-quinazolinamine

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.

Need more information regarding this product? Send us an inquiry: Name: * First Last Company: * E-mail: (if you do not receive a response within 24 hours, please check your email spam folder, as it may have been blocked by your spam filter) * Please specify name of the product: * Word Verification: type_submit_reset_7 SubmitReset