zaprinast
Sign in to saveAlso known as M&B-22948
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.
Research
939 papers- Zaprinast and avanafil increase the vascular endothelial growth factor, vitamin D(3), bone morphogenic proteins 4 and 7 levels in the kidney tissue of male rats applied the glucocorticoid.Archives of physiology and biochemistry · 2022
- Can zaprinast and avanafil induce the levels of angiogenesis, bone morphogenic protein 2, 4 and 7 in kidney of ovariectomised rats?Archives of physiology and biochemistry · 2022
- Phosphodiesterase 5 inhibitors and nitrergic transmission-from zaprinast to sildenafil.European journal of pharmacology · 2001
- Zaprinast activates MAPKs, NFκB, and Akt and induces the expressions of inflammatory genes in microglia.International immunopharmacology · 2012
- Zaprinast, a phosphodiesterase type-5 inhibitor, alters paced mating behavior in female rats.Physiology & behavior · 2009
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Wikidata facts
- Mass
- 271.106925
Show 2 more facts
- canonical SMILES
- CCCOC1=CC=CC=C1C2=NC(=O)C3=NNNC3=N2
- chemical formula
- C₁₃H₁₃N₅O₂
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Article
1 sectionsContents
- 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, 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.