Description
Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.
Trestolone acetate is a synthetic anti-cancer compound that has been shown to inhibit the growth of cancer cells in animal models. It is an estrogen receptor modulator that binds to the estrogen receptor and inhibits its activation by estradiol. Trestolone acetate has also been shown to inhibit the production of inflammatory cytokines, such as tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β), which may be due to its ability to act as a growth factor for immune cells. Trestolone acetate can be used for the treatment of degenerative diseases or bowel disease, such as Crohn's disease. This drug also has a beneficial effect in inflammatory diseases, such as IBD, and autoimmune diseases, such as rheumatoid arthritis. The effective dose is 10 mg/kg body weight per day given orally.
The Rise of MENT - Trestalone
MENT (7alpha-methyl-19-nortestostrone), or trestolone was one of several 19-nortestosterone derivatives to be investigated as a possible male contraceptive therapy due to its unique chemical properties. Initially, drug companies were combining progesterone with testosterone in order to produce a viable male contraceptive option due to progesterone's ability to suppress spermatogenesis.
While testosterone can decrease sperm production, the dose for a test-only birth control would be too high to avoid unwanted side effects.
Testosterone can also convert to DHT via 5alpha-reductase, it can have deleterious effects on the prostate, as well as increase male pattern balding. Since MENT was incapable of binding to 5alpha-reductase and thus cannot convert to DHT, it made it a perfect candidate for an androgen male contraceptive.
The reason for this lies in the unique alpha-methyl group on carbon 7 of the molecule. This methyl group sticks out below the steroidal ring structure and sterically inhibits the conversion to DHT. However, MENT still can undergo aromatization and undergo other androgen-dependent functions, making it effectively act like testosterone in the body despite being a 19-nortestosterone derivative. MENT was also shown to have minimal affinity for the progesterone and mineralocorticoid receptors, despite being a nandrolone derivative.
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