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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).
Cyclic guanosine monophosphate-specific phosphodiesterase type 5 is an enzyme (EC 3.1.4.17) from the phosphodiesterase class. It is found in various tissues, most prominently the corpus cavernosum of the clitoris and of the penis as well as the retina. [5] It has also been recently discovered to play a vital role in the cardiovascular system.
Inhibitors of PDE can prolong or enhance the effects of physiological processes mediated by cAMP or cGMP by inhibition of their degradation by PDE. [13] Sildenafil (Viagra) is an inhibitor of cGMP-specific phosphodiesterase type 5, which enhances the vasodilatory effects of cGMP in the corpus cavernosum and is used to treat erectile dysfunction.
Phosphodiesterase 5 is widely expressed in several tissues in the body for example brain, lung, kidney, urinary bladder, smooth muscle and platelets. [1] It is possible to prevent cGMP hydrolysis by inhibiting PDE5 and therefore treat diseases associated with low cGMP levels, because of this, PDE5 is an ideal target for the development of ...
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Avanafil inhibits phosphodiesterase-5, preventing the degradation of cGMP. [ 10 ] [ 11 ] The increased levels of cGMP causes vasodilation , resulting in an increased blood flow in the penis. [ 11 ] Avanafil's mechanism of action takes places once nitric oxide is released, in association with sexual stimulation.