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Chemical structure of sildenafil (Viagra), the prototypical PDE5 inhibitor. A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplying various tissues.
Phosphodiesterase-5. A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s).
The PDE5 inhibitors sildenafil, vardenafil and tadalafil are competitive and reversible inhibitors of cGMP hydrolysis by the catalytic side of PDE5. The structures of vardenafil and sildenafil are similar, they both contain similar structured purine ring of cGMP that contributes their features to act as a competitive inhibitor of PDE5.
Sildenafil (marketed as Viagra) was the first PDE5 inhibitor on the market. Originally created as a treatment for high blood pressure in 1989, it was found to have a secondary use as an effective PDE5 inhibitor, enabling men who use it to gain stronger erections after arousal. The FDA approved Viagra on March 27, 1998. [20]
This page was last edited on 9 February 2024, at 00:17 (UTC).; Text is available under the Creative Commons Attribution-ShareAlike 4.0 License; additional terms may apply.
The potential for selective phosphodiesterase inhibitors to be used as therapeutic agents was predicted in the 1970s by Weiss and coworkers. [5] This prediction has now come to pass in a variety of fields (e.g. sildenafil as a PDE5 inhibitor and Rolipram as a PDE4 inhibitor).
Pages in category "PDE5 inhibitors" The following 23 pages are in this category, out of 23 total. This list may not reflect recent changes. ...
Avanafil is a PDE5 inhibitor approved for erectile dysfunction by the FDA on April 27, 2012 [2] and by EMA on June 21, 2013. [3] Avanafil is sold under the brand names Stendra and Spedra.