Results 171 to 180 of about 8,073 (209)

PDE5 Inhibitors in the Treatment of LUTS

Current Pharmaceutical Design, 2009
Both 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.
openaire   +2 more sources

Phosphodiesterase Type 5 (PDE5) Inhibitors

2003
Publisher Summary In recent years, the field of Phosphodiesterase Type 5 (PDE5) inhibitors has reached a state of maturity. Standard issues in medicinal chemistry, such as potency, selectivity, physico-chemical properties and oral bioavailability, have been successfully addressed with the known PDE5 inhibitors.
Helmut, Haning, Ulrich, Niewöhner, Erwin, Bischoff   +2 more
openaire   +2 more sources

Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED

Bioorganic & Medicinal Chemistry Letters, 2005
In search of a PDE5 inhibitor for erectile dysfunction, an SAR was developed from a PDE1/PDE5 purine series of leads, which had modest PDE5 potency and poor isozyme selectivity. A compound (41) with PDE5 inhibition and in vivo activity similar to sildenafil was discovered from this effort.
Craig D, Boyle, Ruo, Xu, Theodros, Asberom, Samuel, Chackalamannil, John W, Clader, William J, Greenlee, Henry, Guzik, Yuequing, Hu, Zhiyong, Hu, Claire M, Lankin, Dmitri A, Pissarnitski, Andrew W, Stamford, Yuguang, Wang, Jeffrey, Skell, Stanley, Kurowski, Subbarao, Vemulapalli, Jairam, Palamanda, Madhu, Chintala, Ping, Wu, Joyce, Myers, Peng, Wang   +20 more
openaire   +2 more sources

Conversion of Phosphodiesterase-5 (PDE5) Catalytic Site to Higher Affinity by PDE5 Inhibitors

The Journal of Pharmacology and Experimental Therapeutics, 2007
Phosphodiesterase-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, Roya, Zoraghi, Emmanuel P, Bessay, Alfreda, Beasley, Sharron H, Francis, Jackie D, Corbin   +5 more
openaire   +2 more sources

The Management of Phosphodiesterase-5 (PDE5) Inhibitor Failure

Current Vascular Pharmacology, 2006
The 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, Sashi, Kommu, Faiz H, Mumtaz, Robert J, Morgan, Cecil S, Thompson, Dimitri P, Mikhailidis   +5 more
openaire   +2 more sources

PDE5 Inhibitors: In Vitro and In Vivo Pharmacological Profile

Current Pharmaceutical Design, 2009
PDE5 inhibitors have been clearly established as first-line therapy for the treatment of erectile dysfunction (ED). Three PDE5 inhibitors--sildenafil (Viagra), vardenafil (Levitra) and tadalafil (Cialis)--are currently approved by the FDA and the EMEA for use in ED, whereas sildenafil is also marketed under a different proprietary name (Revatio) for ...
D, Kouvelas, A, Goulas, G, Papazisis, C, Sardeli, C, Pourzitaki   +4 more
openaire   +2 more sources

The Role of PDE5 Inhibitors and the NO/cGMP Pathway in Cancer

Sexual Medicine Reviews, 2016
Phosphodiesterase 5 (PDE5) inhibitors (PDE5i) have been used clinically for the treatment of erectile dysfunction, acting on the nitric oxide/cyclic guanosine monophosphate (NO/cGMP) signaling pathway. Simultaneously, researchers have elucidated the roles that this pathway plays in the regulation of cell proliferation, tumor development, and ...
Taylor C, Peak, Ashley, Richman, Serap, Gur, Faysal A, Yafi, Wayne J G, Hellstrom   +4 more
openaire   +2 more sources

The discovery of novel, potent and selective PDE5 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2001
The design and synthesis of a novel scaffold for potent and selective PDE5 inhibitors are described. Compound 3a was more potent (PDE5 IC50=0.31 nM) and selective (>10,000-fold vs PDE1 and 160-fold selective vs PDE6) PDE5 inhibitor than sildenafil.
Y, Bi, P, Stoy, L, Adam, B, He, J, Krupinski, D, Normandin, R, Pongrac, L, Seliger, A, Watson, J E, Macor   +9 more
openaire   +2 more sources

PDE5 inhibitors: targeting erectile dysfunction in diabetics

Current Opinion in Pharmacology, 2011
Erectile 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
openaire   +2 more sources

Alternative Synthesis of the PDE5 Inhibitor RWJ387273 (R290629)

Synlett, 2007
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Sebastien Lemaire, Bert Willemsens, Istvan E. Marko   +2 more
openaire   +1 more source