fusion protein of wild-type and mutant F163A GAFa domain of enzyme to Green Fluorescent Protein or Renilla luciferase for use in bioluminescence resonance energy transfer assay BRET as a biosensor of cGMP. BRET ratios of wild-type, but not mutant F163A, increase in presence of cGMP, but not cAMP
enzyme inhibitors can reverse the time-dependent forgetting in the object recognition test. The efficacy of the different inhibitors is dependent on the time point of administration after acquisition. Support for a role for cGMP in early stages of memory formation and for cAMP in the late stages of memory formation
enzyme isoform PDE5 mRNA and protein are markedly upregulated in hypertrophied myocardium. Inhibition by sildenafil or MY-5445 significantly increases contractility in hypertrophied myocardium, but not in normal. Protein kinase G is suppressed in hypertrophied myocardium
increased intrarenal isoform PDE5 level mediates the blunted natriuretic response to atrial natriuretic peptide during pregnancy and may contribute to the physiological volume expansion. Atrial natriuretic peptide causes a fall in mean arterial pressure. Intrarenal sildenafil increases the natriuretic response and the rise in fractional excretion of sodium in pregnant rats to the virgin value.
application of 10 mg vardenafil inhibits sphincter of Oddi motility in patients with suspected sphincter of Oddi dysfunction and reduces basal sphincter of Oddi pressure, without significant adverse effects
chronic treatment with a high dose (80 mg/kg) of vardenafil protects the rat bladder from bladder outlet obstruction-induced contractile dysfunction to carbachol
impaired vascular cGMP signalling contributes to the development of diabetic vascular and cardiac dysfunction, which can be prevented by chronic phosphodiesterase-5 inhibition
in end-stage congestive cardiac failure, intravenous sildenafil causes reduction in systemic and pulmonary vascular resistance, sildenafil has a suitable hemodynamic profile for testing of reversibility of secondary pulmonary hypertension in congestive cardiac failure
oral PDE-5 inhibitors improve erectile functioning. PDE-5 inhibitors are more effective than placebo in improving sexual intercourse success. The proportion of men with improved erections is significantly greater among those treated with PDE-5 inhibitors than with placebo
PDE5 inhibition suppresses RhoA/Rho-associated kinase-mediated MMP-2 production by pulmonary artery smooth muscle cells, which may contribute to the regulation of pulmonary vascular remodelling. Thus, PDE5 inhibition may benefit patients with pulmonary hypertension through multiple mechanisms of action
PDE5-inhibitors can improve both lower urinary tract symptoms and erectile dysfunction by targeting various points in the different pathways by increasing cGMP or blocking the effects of norepinephrine and other secondary messengers
peripheral administration of the cGMP-PDE inhibitor zaprinast dramatically alters the inflammatory response of astrocytes and microglia/macrophages to focal brain injury, decreases oxidative stress and neurodegeneration, and increases angiogenesis and vascular endothelial growth factor expression
pharmacological inhibition of PDE5 by vardenafil significantly enhances the endothelium-dependent vasorelaxation in aortic rings rats exposed to peroxynitrite. Acute PDE5-inhibition is advantageous in the treatment of endothelial dysfunction induced by disturbed nitric oxide-cGMP pathway due to nitro-oxidative stress
the combined pharmacotherapy with impaza and PDE5 inhibitors helps to prevent and/or considerably reduces the risk of posttraumatic erectile dysfunction in men with traumas and strictures of the urethra
treatment of mice with vardenafil (5 mg/kg daily for 4 weeks) decreases high density lipoprotein serum levels and the number of antral follicles as well as induces lesser lipid content in luteal cells
convenient and sensitive radioenzymatic assay for characterization and determining the contribution if the various PDE families in cell and tissue, PDE5
convenient and sensitive radioenzymatic assay for characterization and determining the contribution if the various PDE families in cell and tissue, PDE6
convenient and sensitive radioenzymatic assay for characterization and determining the contribution if the various PDE families in cell and tissue, PDE9