Zaprinast
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Names | |
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IUPAC name
5-(2-Propoxyphenyl)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(4H)-one
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Other names
M&B 22,948
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Identifiers | |
37762-06-4 ![]() |
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ChEMBL | ChEMBL28079 ![]() |
ChemSpider | 5520 ![]() |
2919 | |
Jmol 3D model | Interactive image |
PubChem | 5722 |
UNII | GXT25D5DS0 ![]() |
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Properties | |
C13H13N5O2 | |
Molar mass | 271.28 g·mol−1 |
Vapor pressure | {{{value}}} |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references | |
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,[1] selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 μM, respectively.[2][3]
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.[4]
Zaprinast has also been shown to activate the orphan G-protein coupled receptor known as GPR35, both in rats and humans[5] - however the clinical significance of this has yet to be determined.
References
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