150450-53-6 Usage
Uses
MBCQ is a selective inhibitor of cGMP-specific phosphodiesterase.
Biological Activity
mbcq is a cgmp-specific phosphodiesterase pde5 inhibitor.the phosphodiesterase type 5 inhibitor (pde5 inhibitor) is an agent used to inhibit the degradative action of cgmp-specific pde5 on cyclic gmp in the smooth muscle cells lining the blood vessels supplying the corpus cavernosum of the penis. pde5 drugs are used in the treatment of erectile dysfunction and were the first effective oral treatment for this condition. sinve pde5 is also present in the arterial wall smooth muscle within the lungs, pde5 inhibitors have also been applied for the pulmonary hypertension treatment.
in vitro
in previous study, it was found that the addition of mbcq to the blood vessle samples could lead to an 80 to 85% inhibition of pde activity, indicating that most of the activity present in these blood vessels could be attributed to pde5. [1].
in vivo
in animal rat study, tolerance was induced by continuous exposure to glyceryl trinitrate (gtn) for 48 h. results showed that mbcq could significantly decrease the ec(50) values for gtn-induced relaxation in both tolerant and nontolerant tissues, but with the greatest relative shift showing in tolerant veins. moreover, mbcq could also increase the vasodilator potency of a nitric oxide donor (1,1-diethyl-2-hydroxy-2-nitrosohydrazine). a significant increase in cgmp pde activity was found in tolerant femoral vein, whereas pde activity was unchanged in femoral artery [1].
references
[1] macpherson jd, gillespie td, dunkerley ha, maurice dh, bennett bm. inhibition of phosphodiesterase 5 selectively reverses nitrate tolerance in the venous circulation. j pharmacol exp ther. 2006 apr;317(1):188-95.
Check Digit Verification of cas no
The CAS Registry Mumber 150450-53-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,0,4,5 and 0 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 150450-53:
(8*1)+(7*5)+(6*0)+(5*4)+(4*5)+(3*0)+(2*5)+(1*3)=96
96 % 10 = 6
So 150450-53-6 is a valid CAS Registry Number.
150450-53-6Relevant articles and documents
Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
-
, (2008/06/13)
Derivatives of quinazoline are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.
Cyclic GMP Phosphodiesterase Inhibitors. 2. Requirement of 6-Substitution of Quinazoline Derivatives for Potent and Selective Inhibitory Activity
Takase, Yasutaka,Saeki, Takao,Watanabe, Nobuhisa,Adachi, Hideyuki,Souda, Shigeru,Saito, Isao
, p. 2106 - 2111 (2007/10/02)
We synthesized various 4-amino>quinazolines substituted at the 5- to 8-positions and evaluated their inhibitory activities toward cyclic GMP phosphodiesterase (cGMP-PDE) from porcine aorta.Monosubstitution at the 6-position was essential for the inhibitory activity, and the preferred substituents were compact and hydrophobic: methoxy (3b, IC50 = 0.23 μM), methyl (3c, 0.10 μM), chloro (3d, 0.019 μM), thiomethyl (3f, 0.031 μM), and cyano (3p, 0.090 μM) groups.Compounds 3b-d, f, p lacked inhibitory activity toward other PDE isozymes (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).One of these compounds, 3b, elevated the intracellular cGMP level in isolated porcine coronary arteries without causing any change in the cAMP level.We consider that this series of compounds dilates coronary arteries via potent and specific inhibition of cGMP-PDE.
