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Abandoned drugs
Zaprinast
Другие языки:

Zaprinast

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Zaprinast
Zaprinast.svg
Names
IUPAC name
5-(2-Propoxyphenyl)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(4H)-one
Other names
M&B 22,948
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
ECHA InfoCard 100.048.760
PubChem CID
UNII
  • InChI=1S/C13H13N5O2/c1-2-7-20-9-6-4-3-5-8(9)11-14-12-10(13(19)15-11)16-18-17-12/h3-6H,2,7H2,1H3,(H2,14,15,16,17,18,19) checkY
    Key: REZGGXNDEMKIQB-UHFFFAOYSA-N checkY
  • O=C1C2=C(N=NN2)NC(C3=CC=CC=C3OCCC)=N1
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).
☒N verify (what is checkY☒N ?)

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, and to inhibit the mitochondrial pyruvate carrier.



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