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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.
Sildenafil, the first PDE5 inhibitor, was discovered through rational drug design programme. The compound was potent and selective over PDE5 but was lacking preferable pharmacological properties. [40] Structure-activity relationship (SAR) is demonstrated in figure 5, figure 6 and figure 7.
Without sexual stimulation and no activation of the NO/cGMP system, sildenafil should not cause an erection. Studies in vitro have shown that sildenafil is selective for PDE5. [ 21 ] Its effect is more potent on PDE5 than on other known phosphodiesterases (10-fold for PDE6, >80-fold for PDE1, >700-fold for PDE2, PDE3, PDE4, PDE7, PDE8, PDE9 ...
PDE5 normally breaks down cGMP, which is responsible for arterial smooth muscle relaxation. ... and other phosphodiesterase type 5 inhibitors, Viagra should be prescribed and taken under the ...
This is thanks to an enzyme called phosphodiesterase type 5 (PDE5). Viagra inhibits PDE5 and acts as a vasodilator (something that dilates blood vessels and increases blood flow).
Sildenafil is most commonly prescribed to be taken one time per day in doses between 25 and 100 mg for ED. Your healthcare provider will determine the best dosage for you based on a number of factors.
Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum. The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binding agent of PDE5 in the corpus cavernosum, resulting in more cGMP and increased ...
As the name suggests, PDE5 inhibitors inhibit PDE5, which degrades cGMP. So when you take Viagra, cGMP builds up in the smooth muscle and is free to do its thing — which is to dilate blood ...
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