Zaprinast
Zaprinast structure
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Common Name | Zaprinast | ||
|---|---|---|---|---|
| CAS Number | 37762-06-4 | Molecular Weight | 271.275 | |
| Density | 1.484g/cm3 | Boiling Point | 406.3±47.0 °C at 760 mmHg | |
| Molecular Formula | C13H13N5O2 | Melting Point | 237-238ºC dec. | |
| MSDS | Chinese USA | Flash Point | 199.5±29.3 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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Metabolomics analysis of metabolic effects of nicotinamide phosphoribosyltransferase (NAMPT) inhibition on human cancer cells.
PLoS ONE 9(12) , e114019, (2014) Nicotinamide phosphoribosyltransferase (NAMPT) plays an important role in cellular bioenergetics. It is responsible for converting nicotinamide to nicotinamide adenine dinucleotide, an essential molecule in cellular metabolism. NAMPT has been extensively stud... |
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Inhibition of mitochondrial pyruvate transport by zaprinast causes massive accumulation of aspartate at the expense of glutamate in the retina.
J. Biol. Chem. 288(50) , 36129-40, (2013) Transport of pyruvate into mitochondria by the mitochondrial pyruvate carrier is crucial for complete oxidation of glucose and for biosynthesis of amino acids and lipids. Zaprinast is a well known phosphodiesterase inhibitor and lead compound for sildenafil. ... |
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GPR35 activation reduces Ca2+ transients and contributes to the kynurenic acid-dependent reduction of synaptic activity at CA3-CA1 synapses.
PLoS ONE 8 , e82180, (2013) Limited information is available on the brain expression and role of GPR35, a Gi/o coupled receptor activated by kynurenic acid (KYNA). In mouse cultured astrocytes, we detected GPR35 transcript using RT-PCR and we found that KYNA (0.1 to 100 µM) decreased fo... |
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Phosphodiesterase inhibition induces retinal degeneration, oxidative stress and inflammation in cone-enriched cultures of porcine retina
Exp. Eye Res. 111 , 122-33, (2013) Inherited retinal degenerations affecting both rod and cone photoreceptors constitute one of the causes of incurable blindness in the developed world. Cyclic guanosine monophosphate (cGMP) is crucial in the phototransduction and, mutations in genes related to... |
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Galpha(i2) inhibition of adenylate cyclase regulates presynaptic activity and unmasks cGMP-dependent long-term depression at Schaffer collateral-CA1 hippocampal synapses.
Learn. Mem. 15 , 261-70, (2008) Cyclic AMP signaling plays a central role in regulating activity at a number of synapses in the brain. We showed previously that pairing activation of receptors that inhibit adenylate cyclase (AC) and reduce the concentration of cyclic AMP, with elevation of ... |
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An intact medial preoptic area is necessary for zaprinast to modulate paced mating behavior in female rats
Physiol. Behav. 105(2) , 264-8, (2012) The present study examined the interaction between the regulation of paced mating behavior by the medial preoptic area (mPOA) and by the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) pathway, as modulated by zaprinast, a phosphodiesterase inhibitor.... |
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Effect of the phosphodiesterase-5 inhibitor zaprinast on ischemia-reperfusion injury in rats.
J. Endourol. 27(3) , 338-42, (2013) The cardiac and renal protective effects of phosphodiesterase-5 (PDE-5) inhibitors against ischemia-reperfusion injury have recently been demonstrated in animal studies. We evaluated the effect of pretreatment with the PDE-5 inhibitor zaprinast on warm renal ... |
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Association of ex vivo vascular and bronchial dysfunctions in smokers.
Pulm. Pharmacol. Ther. 24(2) , 227-31, (2011) It has recently been shown that systemic endothelial dysfunction is associated with airflow limitation in COPD. We conducted this ex vivo study to assess whether endothelial dysfunction of pulmonary arteries of former smokers was associated with modifications... |
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Neuronal nitric oxide synthase supports Renin release during sodium restriction through inhibition of phosphodiesterase 3.
Am. J. Hypertens. 23(11) , 1241-6, (2010) Mice with targeted deletion of neuronal nitric oxide (NO) synthase (nNOS⁻(/)⁻) display inability to increase plasma renin concentration (PRC) in response to sodium restriction. nNOS has a distinct expression at the macula densa (MD), and in the present study,... |
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Phosphodiesterase 5 inhibitors and nitrergic transmission-from zaprinast to sildenafil.
Eur. J. Pharmacol. 411(1-2) , 1-10, (2001) Phosphodiesterase 5 terminates the cellular actions of the second messenger molecule cyclic GMP; inhibitors of phosphodiesterase 5 will therefore increase and prolong the actions of endogenous substances that signal via the cyclic GMP pathway, including nitri... |