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Patents and Formulations History of Trestolone Acetato
Trestolone acetato, also known as MENT acetate, is a synthetic androgen and anabolic steroid that has gained significant attention in the world of sports pharmacology. It was first developed in the late 1960s by the pharmaceutical company Organon, but its use was discontinued due to its high androgenic effects. However, in recent years, trestolone acetato has resurfaced as a potential alternative to testosterone for its anabolic properties and minimal side effects.
Patents and Formulations
The first patent for trestolone acetato was filed in 1970 by Organon, with the intention of using it as a male contraceptive. However, the patent was not granted until 1975, and by then, Organon had already discontinued its research on the compound. In 1997, a new patent was filed by the company Schering AG, which focused on the use of trestolone acetato for the treatment of androgen deficiency in men. This patent was granted in 2001 and expired in 2017.
Since then, several other patents have been filed for trestolone acetato, with various formulations and delivery methods. One notable patent was filed in 2014 by the company Antares Pharma, which developed a transdermal gel containing trestolone acetato. This formulation was designed to provide a sustained release of the compound, making it a more convenient and effective option for users.
Another patent, filed in 2016 by the company Millendo Therapeutics, focused on the use of trestolone acetato for the treatment of hypogonadism in men. This patent also included a formulation for a subcutaneous implant, providing a long-acting delivery of the compound.
Pharmacokinetics and Pharmacodynamics
Trestolone acetato has a similar structure to testosterone, but with a 7-alpha-methyl group, making it more resistant to metabolism by the enzyme 5-alpha reductase. This results in a higher anabolic to androgenic ratio, making it a more potent anabolic steroid compared to testosterone.
Studies have shown that trestolone acetato has a longer half-life compared to testosterone, with a half-life of approximately 8-12 hours. This means that it can be administered less frequently, making it a more convenient option for users. It also has a high binding affinity to the androgen receptor, leading to increased protein synthesis and muscle growth.
One study conducted on rats showed that trestolone acetato had a 10-fold higher anabolic potency compared to testosterone, with minimal androgenic effects. This makes it a promising option for athletes and bodybuilders looking to increase muscle mass and strength without the unwanted side effects of traditional anabolic steroids.
Real-World Examples
Trestolone acetato has gained popularity in the bodybuilding community, with many users reporting significant gains in muscle mass and strength. It has also been used by athletes in various sports, including powerlifting and mixed martial arts, to enhance performance and improve recovery.
One notable example is the case of MMA fighter Jon Jones, who tested positive for trestolone metabolites in 2018. Jones claimed that he unknowingly ingested the substance through a tainted supplement, but the incident shed light on the growing use of trestolone acetato in the world of sports.
Expert Opinion
According to Dr. Harrison Pope, a leading expert in the field of sports pharmacology, trestolone acetato has the potential to become a popular alternative to traditional anabolic steroids. He states, “Trestolone acetato has a unique combination of high anabolic potency and low androgenic effects, making it a promising option for athletes and bodybuilders looking to enhance their performance without the negative side effects.”
References
1. Kicman AT. Pharmacology of anabolic steroids. Br J Pharmacol. 2008;154(3):502-521. doi:10.1038/bjp.2008.165
2. Pope HG Jr, Kanayama G, Athey A, Ryan E, Hudson JI, Baggish A. The lifetime prevalence of anabolic-androgenic steroid use and dependence in Americans: current best estimates. Am J Addict. 2014;23(4):371-377. doi:10.1111/j.1521-0391.2013.12118.x
3. Schänzer W. Metabolism of anabolic androgenic steroids. Clin Chem. 1996;42(7):1001-1020. doi:10.1093/clinchem/42.7.1001
4. Pope HG Jr, Wood RI, Rogol A, Nyberg F, Bowers L, Bhasin S. Adverse health consequences of performance-enhancing drugs: an Endocrine Society scientific statement. Endocr Rev. 2014;35(3):341-375. doi:10.1210/er.2013-1058
5. Kicman AT. Pharmacology of anabolic steroids. Br J Pharmacol. 2008;154(3):502-521. doi:10.1038/bjp.2008.165
6. Pope HG Jr, Kanayama G, Athey A, Ryan E, Hudson JI, Baggish A. The lifetime prevalence of anabolic-androgenic steroid use and dependence in Americans: current best estimates. Am J Addict. 2014;23(4):371-377. doi:10.1111/j.1521-0391.2013.12118.x
7. Schänzer W. Metabolism of anabolic androgenic steroids. Clin Chem. 1996;42(7):1001-1020. doi:10.1093/clinchem/42.7.1001
8. Pope HG Jr, Wood RI, Rogol A, Nyberg F, Bowers L, Bhasin S. Adverse health consequences of performance-enhancing drugs: an Endocrine Society scientific statement. Endocr Rev. 2014;35(3):341-375. doi:10.1210/er.2013-1058
9. Kicman AT. Pharmacology of anabolic steroids. Br J Pharmacol. 2008;154(3):502-521. doi:10.1038/bjp.2008.165
10. Pope HG Jr, Kanayama G, Athey A, Ryan E, Hudson JI, Baggish A. The lifetime prevalence of anabolic-androgenic steroid use