Results 181 to 190 of about 12,266 (204)
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PDE5 inhibitors: targeting erectile dysfunction in diabetics
Current Opinion in Pharmacology, 2011Erectile dysfunction (ED) is strongly linked to cardiovascular disease (CVD), especially in diabetics. ED is associated with deleterious changes in the overall vasculature and is recognized as an indicator of higher risk for adverse cardiovascular events.
Sharron H, Francis, Jackie D, Corbin
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Conversion of Phosphodiesterase-5 (PDE5) Catalytic Site to Higher Affinity by PDE5 Inhibitors
The Journal of Pharmacology and Experimental Therapeutics, 2007Phosphodiesterase-5 (PDE5) specifically hydrolyzes cGMP, thereby contributing to modulation of intracellular levels of this nucleotide. In the present study, preincubation with cGMP increased PDE5 catalytic activity for cGMP degradation, and it converted the PDE5 catalytic site to a form that was more potently inhibited by each of the three PDE5 ...
Mitsi A, Blount +5 more
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Alternative Synthesis of Tadalafil: PDE5 Inhibitor
Synthetic Communications, 2008Abstract Two-step alternative synthesis of tadalafil (1) is described. The synthesis features Pictet–Spengeler type reaction and DCC (N,N′-dicyclohexylcarbodiimide)/HOBt (N-hydroxybenzotriazole)–mediated double amidation employing sarcosine ethyl ester hydrochloride.
Raghupathi Reddy Anumula +7 more
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The efficacy and safety of PDE5 inhibitors
Clinical Cornerstone, 2005Inhibition of phosphodiesterase-5 (PDE5) reduces the degradation of cyclic guanosine monophosphate, which allows erectile function to occur by relaxation of penile smooth muscle. Three PDE5 inhibitors (sildenafil, tadalafil, and vardenafil) in a range of doses are available.
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High lung PDE5: A strong basis for treating pulmonary hypertension with PDE5 inhibitors
Biochemical and Biophysical Research Communications, 2005[3H]Vardenafil (Levitra) or [3H]tadalafil (Cialis) binding was used to quantify PDE5 in rat lung and heart tissue. Each radioligand bound to purified recombinant phosphodiesterase-5 (PDE5) or to PDE5 in crude extracts with strong affinity, high specificity, slow dissociation, and good stoichiometry.
Jackie D, Corbin +3 more
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PDE5 Inhibitors in the Treatment of LUTS
Current Pharmaceutical Design, 2009Both lower urinary tract symptoms (LUTS) and erectile dysfunction (ED) have a negative impact on patients' quality of life. The co-prescription of two active agents for these conditions will improve each condition and the addition of one drug to the other may potentiate the primary response of the first treatment and thereby improve the QoL of patients.
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The Management of Phosphodiesterase-5 (PDE5) Inhibitor Failure
Current Vascular Pharmacology, 2006The oral phosphodiesterase type 5 (PDE5) inhibitors have made a valuable contribution to the treatment of erectile dysfunction (ED). PDE5 inhibitors enhance cavernosal smooth muscle relaxation, vasodilatation and penile erection. However, PDE5 inhibitors are not always effective.
David H W, Lau +5 more
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Cardiovascular safety of PDE5 inhibitors.
The Canadian journal of urology, 2003Erectile dysfunction (ED) and cardiovascular disease share many of the same risk factors and have some common elements of pathophysiology. Clinically, they often coexist. Another link between the two conditions is that sildenafil, the first oral therapeutic agent effective in treating ED, has been shown to potentiate the hypotensive effects of nitrates,
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The Hemodynamics of Phosphodiesterase-PDE5 Inhibitors
2004Sildenafil citrate (Viagra™; Pfizer, Inc., New York, NY) is the first of a series of orally active phosphodiesterase (PDE) type-5 inhibitors that have and will continue to transform the treatment of erectile dysfunction (ED) (1). Initially advocated as a potential alternative to oral nitrates for the treatment of stable angina pectoris, sildenafil’s ...
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Structure -activity relationships of PDE5 inhibitors.
Current medicinal chemistry, 2008cGMP has a short-term effect on smooth muscle tone and a longer-term effect on responses to chronic drug treatment or proliferative signals. cGMP-Phosphodiesterase type 5 (PDE5) hydrolizes cGMP, and the result is smooth muscle contraction. PDE5 is a relatively novel therapeutic target of various diseases, such as erectile dysfunction and pulmonary ...
D, Eros +6 more
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