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Drug history and how it works


The formula Sildenafil, the active ingredient in The Little Blue Pill, was originally tested to treat heart-related conditions such as High Blood Pressure, Angina and Hypertension.
Scientists soon discovered it actually worked better as a treatment for Erectile Dysfunction.

The mechanism of action of Sildenafil involves the protection of Cyclic Guanosine MonoPhosphate (cGMP) from degradation, by cGMP-specific PhosphoDiEsterase type 5 (PDE5) in the Corpus Cavernosum (penis).

There are 11 PDE's found in the body.
Erectile Dysfunction (ED) is caused by PDE5 working against (decomposing) cGMP.
PDE5 is an enzyme that accepts cGMP and breaks it down.
If a drug can inhibit PDE5, the result would assist the cGMP to produce firmer erections. The chemical Sildenafil, fits right into the PDE5 enzyme and disables it.
The drug is rapidly absorbed in the small intestine within a few minutes of swallowing with a glass of water. Naturally dispersed throughout the body's system, it's finally washed out of the blood, by the liver and kidneys.

So What does the drug do, exactly?
There are at least three ways to achieve greater/lasting erections :~
Increase the amount of Nitric Oxide produced in the penis.
Increase the amount of cGMP produced in the penis in response to the Nitric Oxide.
Eliminate the PDE in the penis so that the cGMP builds up instead of getting decomposed by the PDE.

The Little Blue Pill employs the later solution - by eliminating the PDE responsible for decomposing the cGMP. This way, the cGMP is able to build within the penis, resulting in an increased effect on the artery walls.
The greater the cGMP the greater the blood flow, so, the greater the blood flow, the greater the degree of an erection.
This method targets PDE5, which is primarily found in the penis. Once this was realised, the development of the drug Viagra® was relatively simple.

Sildenafil is a potent and selective inhibitor of cGMP-specific PhosphoDiEsterase type 5 (PDE5), which is responsible for degradation of cGMP in the penis.
Sildenafil works by inhibiting PhosphoDiEstrase-5, an enzyme which degrades Cyclic Guanosine MonoPhosphate (cGMP) a cell messenger that causes the blood vessels to relax.
In action, it resembles Cyclic Guanosine MonoPhosphate (the substrate)(cGMP) and binds to the active site of PhosphoDiEsterase type 5 (PDE5).

By inhibiting the enzyme, the drug allows greater widening of the blood vessels (vasodilation) and greater blood flow.

Et Voilà! as with many laboratory discoveries, a scientific serendipitous moment, produced a magical solution to a significant problem, for tens of millions of men worldwide.

After all the science, to sum up in simple terms, the message is easy to understand, take just one tablet, wait a short while, start getting down and dirty with your partner, and presto, you will have a hard-on to be utterly proud of the little blue pill ~ smile

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Sildenafil :~ (molecule UK-92-480)
1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenylsulfonyl]-4-methylpiperazine

Chemical formula :~
C22H30N6O4S

the little blue pill ~ formula