Nolvadex / tamoxifen belongs to a category and class of drugs known as selective Estrogen receptor modulators (SERMs). Selective Estrogen receptor modulators belong to an even broader class of drugs known as anti-estrogens. The other subcategory of drug under the anti-estrogens category is known as aromatase inhibitors (AIs), such as Aromasin (Exemestane) and Arimidex (Anastrozole). AIs and SERMs make up anti-estrogens. Aromatase inhibitors differ greatly from SERMs in their action and how they deal with the issues of estrogen control. The misunderstanding that SERMs, such as Nolvadex and clomid, serve to lower estrogen levels must first be addressed before delving into any further details. This is a persistent rumor among the anabolic steroid using community that has begun to erode as of late, but the rumor still persists. SERMs serve to block the action of Estrogen at the receptor sites in breast tissue by occupying the receptor sites in place of Estrogen so that Estrogen itself cannot exert its effects there through receptor site binding. Conversely, SERMs will also act as Estrogens at receptor sites at other cells in other areas of the body (the liver, for example in Nolvadex’s case). SERMs do not lower circulating levels of Estrogen in blood plasma. Aromatase inhibitors serve to do this by eliminating the production of Estrogen through binding to and disabling the aromatase enzyme, which is the enzyme responsible for the conversion (or aromatization) of androgens into Estrogen.
It has already been established that Nolvadex, being a SERM, does not reduce circulating Estrogen levels in the body, but instead serves to occupy the receptor sites in breast tissue so that Estrogen itself cannot bind to these receptors due to Nolvadex’s stronger binding strength to it. In layman’s terms, Nolvadex essentially acts as a ‘fake’ Estrogen that acts as a placeholder at the receptor sites in breast tissue. As a result, Estrogen cannot activate gene transcription in the cells there in order to formulate gynecomastia, and any existing Estrogen that has already bound to receptor sites will essentially be ‘forced’ out of the receptor sites by Nolvadex which then occupies the receptor site instead. This is very promising news for anabolic steroid using individuals that wish to eliminate and reverse formulating gynecomastia in its early stages, as well as for those individuals very sensitive to the gynecomastia side effect of rising Estrogen levels that might wish to utilize Nolvadex as a preventative measure. This is the primary purpose and function of Nolvadex, and is the primary desired effect that anabolic steroid using bodybuilders and athletes utilize it for. Nolvadex will not serve to block or reduce any other Estrogenic side effects, however, as it serves only to block Estrogenic activity at the breast tissue area (when major Estrogenic side effects are concerned). Nolvadex does not (nor do any SERMs) serve to reduce bloating, water retention, rising blood pressure (as a result of water retention), or acne formation – these are all side effects resultant from increasing blood plasma Estrogen levels.
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