Zaprinast
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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 | |
3D model (
JSmol ) |
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ChEMBL | |
ChemSpider | |
ECHA InfoCard
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100.048.760 |
IUPHAR/BPS |
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PubChem CID
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UNII | |
CompTox Dashboard (EPA)
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Properties | |
C13H13N5O2 | |
Molar mass | 271.280 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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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
P. falciparum cGMP-specific phosphodiesterase, with an IC50 value of 3.8 μM.[4]
Zaprinast has also been shown to activate the orphan
pyruvate carrier. [6]
References