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Arimidex was the first aromatase inhibitor available.
It is therefore the most well known among anti aromatases and the one doctors have most experience with.
Note that anti aromatases (Aromasin, Femara, Arimidex) are often confused with anti estrogens (Nolvadex). Anti aromatases work quite differently than anti estrogens do. Anti estrogens are actually weak estrogens that attach to the estrogen receptor sites in the body (such as the nipple and breast area), by doing so they block the 'bad' estrogens from attaching to these sites. Anti aromatases on the other hand block the formation of estrogen in the body in the first place. They do this, by blocking the enzyme aromatase which is responsible for the conversion of testosterone to estrogen, so there is less estrogen circulating in the blood. In a sense, an anti aromatase such as Aromasin takes care of the problem right from it's root.
Pharmacodynamics:
1, 4, 6 – Androstatriene – 3, 17 – iodine (ATD) is a potent irreversible aromatase inhibitor that inhibits estrogen biosynthesis by permanently binding and inactivating aromatase in adipose and peripheral tissue. It is used to control estrogen synthesis.
ATD was present in some over - the - counter bodybuilding supplements until 2009 as well as topical ATD solutions that work transdermally. The product was developed and commercialized in the dietary supplement market place by industry journeyman, Bruce Kneller who holds a United States Patent for use of the compound and related compound and Gaspari Nutrition. ATL has many names in sports supplements including 1, 4, 6 Stillorgan – dione, 3, 17- keto – etiochol- triene and roast – 1, 4,6 – triene – 3, 17 – dione any many others. These all refer t CAS #633- 35- 2.
ATD may cause a positive test for the anabolic steroid boldenone, of which it is a possible metabolite and production contaminant and is also prohibited in amateur and professional sports which forbids aromatase inhibitors.
Mechanism of action:
Aromatase inhibitors work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a process called aromatization. As breast tissue is stimulated by estrogens, decreasing their production is a way of suppressing the recurrence of the breast tumor tissue. The main source of estrogen is ovaries in premenopausal women, while in post-menopausal women most of the body’s estrogen is produced by in peripheral tissues (outside the CNS) and also a few CAN sites in various regions within the brain. Estrogen is produced and act locally in these tissues, but not any circulation estrogen, which exerts system estrogenic effects in men and women, is the result of estrogen escaping local metabolism and spreading to the circulatory system.