CAS: 37762-06-4 | ZAPRINAST

Synonyms：
2-(2-PROPYLOXYPHENYL)-8-AZAPURIN-6-ONE;
B 22,948;
2-o-propoxyphenyl-8-azapurin-6-one;
8-Aza-2-(2-propoxyphenyl)-6-purinone;
Potassium phosphate monobasic;
3,6-dihydro-5-(2-propoxyphenyl);
1,4-Dihydro-5-(2-propoxyphenyl)-7H-1,2,3-triazolo(4,5-d)pyrimidin-7-one;
Phenylaza purinon;
2-(2-Propoxyphenyl)-8-azahypoxanthine;

Application：
Zaprinast was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which successfully reached the market. It is a phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 μM, respectively.
Zaprinast inhibits the growth of asexual blood-stage malaria parasites (P. falciparum) in vitro with an ED50 value of 35 μM, and inhibits PfPDE1, a P. falciparum cGMP-specific phosphodiesterase, with an IC50 value of 3.8 μM.
Zaprinast has also been shown to activate the orphan G-protein coupled receptor known as GPR35, both in rats and humans - however the clinical significance of this has yet to be determined.

It is often used to study the release and mechanism of neurotransmitters, especially in the study of smooth muscle relaxation, vasodilation, and the treatment of obstructive pulmonary hypertension. In addition, it can also be used to treat other related diseases such as cardiovascular disease, obstructive pulmonary disease and chronic obstructive pulmonary disease.

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