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zaprinast : ウィキペディア英語版
zaprinast

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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, 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.
==References==



抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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