PURPOSE Phosphodiesterase (PDE) inhibitors are important therapeutic agents, but their effects on photoreceptor PDE (PDE6) and photoreceptor cells are poorly understood. The potency and selectivity of various classes of PDE inhibitors on purified rod and cone PDE6 and on intact rod outer segments (ROS) were characterized. METHODS The inhibition constant (K(i)) of isozyme-selective PDE inhibit...

Non-selective beta-blockers are the mainstay of medical therapy for portal hypertension in liver cirrhosis. Inhibitors of phosphodiesterase-5 (PDE-5-inhibitors) reduce portal pressure in the acute setting by > 10% which may suggest a long-term beneficial effect. Currently, there is no available data on long-term treatment of portal hypertension with PDE-5-inhibitors. This case of a patient with...

A highly potent inhibitor of calmodulin-sensitive phosphodiesterase (PDE) activity was isolated from the culture broth of an unidentified fungal isolate, SCF-125. A chemically defined medium was developed for production of this compound. The PDE inhibitor was isolated from the fermentation filtrate by adsorption on a macro-reticular resin and further purified by gel filtration chromatography an...

In this study, we aimed to investigate the peripheral antinociception effects of specificphosphodiesterase 5 (PDE-5) inhibitor vardenafil on carrageenan-induced nociception in rats,and the role of calcium besides the L-arginine- nitric oxide (NO)- cyclic guanosine monophophate(cGMP) pathway in these effects. Hyperalgesia was induced by the intraplantar injection of 0.1mL fresh carrageenan solut...

PURPOSE cAMP phosphodiesterase (PDE) 4 is a family of enzymes the inhibition of which induces chronic lymphocytic leukemia (CLL) apoptosis. However, leukemic cells from a subset of CLL patients are relatively resistant to treatment with the PDE4 inhibitor rolipram, particularly when this drug is used in the absence of an adenylate cyclase stimulus such as forskolin. Elevated cAMP levels induce ...

BACKGROUND The anti-inflammatory effects of the selective phosphodiesterase (PDE) inhibitors cilostazol (PDE 3), RO 20-1724 (PDE 4) and sildenafil (PDE 5) were examined in a murine model of allergic asthma. These compounds were used alone and in combination to determine any potential synergism, with dexamethasone included as a positive control. METHODS Control and ovalbumin sensitised Balb/C ...

CASE A 45-year-old man has a 10-year history of migraine without aura occurring about once a week relieved by an oral triptan. When he sought treatment for erectile dysfunction from a urologist, the side effect of triggering migraine was brought up. Now the patient and the urologist want my opinion about whether the patient should try an oral phosphodiesterase-5 inhibitor (PDE-5) and, if so, do...

In this study, we aimed to investigate the peripheral antinociception effects of specificphosphodiesterase 5 (PDE-5) inhibitor vardenafil on carrageenan-induced nociception in rats,and the role of calcium besides the L-arginine- nitric oxide (NO)- cyclic guanosine monophophate(cGMP) pathway in these effects. Hyperalgesia was induced by the intraplantar injection of 0.1mL fresh carrageenan solut...