Titre du document / Document title

Phosphodiesterase type 5 inhibitors : Molecular pharmacology and interactions with other phosphodiesterases : Sexual medicine research-PDE5 inhibitors and beyond

Auteur(s) / Author(s)

SEFTEL Allen D. ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Urology, Case Western Reserve University, School of Medicine, 11100 Euclid Ave, Cleveland, Ohio 44106-5046, ETATS-UNIS

Résumé / Abstract

Erectile function is determined by tight regulation of relaxation or contraction of corpus cavernosal smooth muscle, which is the result of a long and complex chain of molecular events. Control of erectile function resides in signaling pathways of the central and peripheral nervous system, as well as intracellular events in the penile smooth muscle. Vascular events resulting in erection have long been understood, and the role of the signaling pathways of the central and peripheral nervous systems in erectile function and dysfunction has become increasingly clear over the last decade. This knowledge has led to the development and current availability of effective oral treatments for erectile dysfunction, the selective phosphodiesterase type 5 (PDE5) inhibitors-sildenafil, vardenafil and tadalafil. In the past few years we have seen an elucidation of the molecular events involved in erectile function and dysfunction and the detailed mechanisms of action by which the specific PDE5 inhibitors work. A review of those mechanisms helps to explain the success of the currently available PDE5 inhibitors and the differences between them and suggests new approaches for developing potential future novel therapies or refinements to existing structures that may improve their efficacy, selectivity and safety profiles.

Revue / Journal Title

Current pharmaceutical design   ISSN 1381-6128 

Source / Source

2005, vol. 11, n^o31, pp. 4047-4058 [12 page(s) (article)] (43 ref.)

Langue / Language

Anglais

Editeur / Publisher

Bentham, Sharjah, EMIRATS ARABES UNIS  (1995) (Revue)

Mots-clés anglais / English Keywords

Carboline derivatives ; Male genital diseases ; Enzyme ; Hydrolases ; Esterases ; Phosphoric diester hydrolases ; Phosphodiesterase 5 inhibitor ; Vasodilator agent ; Enzyme inhibitor ; Tadalafil ; Vardenafil ; Mechanism of action ; Erection disorders ; Sildenafil ; Molecular interaction ; 3',5'-Cyclic-GMP phosphodiesterase ;

Mots-clés français / French Keywords

Carboline dérivé ; Appareil génital mâle pathologie ; Enzyme ; Hydrolases ; Esterases ; Phosphoric diester hydrolases ; Inhibiteur phosphodiestérase 5 ; Vasodilatateur ; Inhibiteur enzyme ; Tadalafil ; Vardénafil ; Mécanisme action ; Erection pathologie ; Sildénafil ; Interaction moléculaire ; 3',5'-Cyclic-GMP phosphodiesterase ;

Mots-clés espagnols / Spanish Keywords

Aparato genital macho patología ; Enzima ; Hydrolases ; Esterases ; Phosphoric diester hydrolases ; Inhibidor fosfodiesterasa 5 ; Vasodilatador ; Inhibidor enzima ; Tadalafilo ; Vardenafil ; Mecanismo acción ; Erección patología ; Sildenafilo ; Interacción molecular ; 3',5'-Cyclic-GMP phosphodiesterase ;

Mots-clés d'auteur / Author Keywords

Erectile dysfunction ; PDE5 ; PDE5 inhibitors ; mechanism of action ; molecular interactions ; biochemistry ; physiology ; pharmacology ;

Localisation / Location

INIST-CNRS, Cote INIST : 26320, 35400012138237.0060