Although this steroid is strongly androgenic, the anabolic effect of it is considered too weak for muscle building purposes. This is due to the fact that Proviron is rapidly reduced to inactive metabolites in muscle tissue, a trait also characteristic of dihydrotestosterone. The belief that the weak anabolic nature of this compound indicated a tendency to block the androgen receptor in muscle tissue, thereby reducing the gains of other more potent muscle building steroids, should likewise not be taken seriously. In fact due to its extremely high affinity for plasma binding proteins such as SHBG, Proviron may actually work to increase the activity of other steroids by displacing a higher percentage into a free, unbound state. Among athletes Proviron is primarily used as an anti-estrogen. It is believed to act as an anti-aromatase in the body, preventing or slowing the conversion of steroids into estrogen. The result is somewhat comparable to Arimidex (though less profound), the drug acting to prevent the buildup of estrogen in the body. This is in direct contrast to Nolvadex , which only blocks the ability of estrogen to bind and activate receptors in certain tissues. The anti-aromatization effect is preferred, as it is a more direct and efficient means of dealing with the problem of estrogenic side effects. Another disadvantage of Nolvadex is that if discontinued too early, a rebound effect may occur as high serum estrogen levels are again free to take action. This of course could mean a rapid onset of side effects such as gynecomastia. Most actually prefer to use both Proviron and Nolvadex, especially during strongly estrogenic cycles. With each item attacking estrogen at a different angle, side effects are often greatly reduced.
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Proviron has four distinct uses in the world of bodybuilding. The first being the result of its structure. It is 5-alpha reduced and not capable of forming estrogen, yet it nonetheless has a much higher affinity for the aromatase enzyme (which converts testosterone to estrogen) than testosterone does. That means in administering it with testosterone or another aromatizable compound, it prevents estrogen build-up because it binds to the aromatase enzyme very strongly, thereby preventing these steroids from interacting with it and forming estrogen. So Mesterolone use has the extreme benefit of reducing estrogenic side-effects and water retention noted with other steroids, and as such still help to provide mostly lean gains. Its also been suggested that it may actually downgrade the actual estrogen receptor making it doubly effective at reducing circulating estrogen levels.