4 Chlorodehydromethyle Testosterone

Testosterone derivatives and related compounds (such as anabolic-androgenic steroids—AAS) are frequently misused by athletes (both professional and amateur) wishing to promote muscle development and strength or to cover AAS misuse. Even though these agents are vastly regarded as abusive material, they have important pharmacological activities that cannot be easily replaced by other drugs and have therapeutic potential in a range of conditions (e.g., wasting syndromes, severe burns, muscle and bone injuries, anemia, hereditary angioedema). Testosterone and related steroids have been in some countries treated as controlled substances, which may affect the availability of these agents for patients who need them for therapeutic reasons in a given country. Although these agents are currently regarded as rather older generation drugs and their use may lead to serious side-effects, they still have medicinal value as androgenic, anabolic, and even anti-androgenic agents. This review summarizes and revisits the medicinal use of compounds based on the structure and biological activity of testosterone, with examples of specific compounds. Additionally, some of the newer androgenic-anabolic compounds are discussed such as selective androgen receptor modulators, the efficacy/adverse-effect profiles of which have not been sufficiently established and which may pose a greater risk than conventional androgenic-anabolic agents.

Keywords: androgen receptor, antiandrogens, aging, longevity, medicinal natural products, performance-enhancing drugs, selective androgen receptor modulators, testosterone

Testosterone (T) derivatives and their (semi-)synthetic analogues (so-called androgenic anabolic steroids—AAS) have been controversial for already quite some time. These substances have become the subject of abuse by professional athletes, and currently also by a significant number of amateur athletes, to enhance performance (i.e., performance-enhancing drugs) and body aesthetics. However, T and many AAS have valuable and often irreplaceable pharmacological activities that are medicinally useful, though these compounds are currently regarded as rather older generation drugs.

T and related compounds primarily act as androgens, promoting the development and maintenance of male sex characteristics such as maturation of the sex organs, voice deepening, and growth of facial and body hair. They also have an anabolic activity that promotes the storage of protein and stimulates the growth of bone and muscles, and these functions are especially important from a medicinal standpoint [1]. Indeed, tremendous efforts have been put into developing agents with increased anabolic activity such as the recently discovered selective androgen receptors modulators (SARMs). However, there is still no single anabolic molecule from which the androgenic activity has been fully eliminated. T and other AAS still find their use in the treatment of a wide range of human diseases, including hypogonadism, male sexual impotence, and some types of breast cancer in women.