Selective Androgen Receptor Modulators (SARMs) in Sports: A Review

Selective androgen receptor modulators (SARMs) are an exciting group of molecules with pronounced anabolic effects and very weak to missing androgenic ones. This is due to the tissue selectivity they possess and is their big advantage over anabolic androgenic steroids (AAS). As a result of this SARMs tend to be a big promise for improving the treatment process in different socially significant diseases such as osteoporosis, muscle wasting, benign prostatic hyperplasia, hypogonadism, sexual dysfunction, neurodegenerative diseases etc. SARMs are included in the prohibited list of World Anti-Doping agency (WADA) as they are a temptation for a lot of athletes regarding the exerted strong anabolic effect. However, as SARMs are freely available on the internet there are some reports for positive doping tests in professional sports connected with them. Still further research is needed to examine all the side effects of SARMs. Some of them may be harmful so both professional and amateur sportsmen, their coaches and doctors should be informed about this interesting topic. Keywords: SARM(s), anabolic effect, sports, doping, side effects

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Myoanabolic steroids and selective androgen receptor modulators: mechanism of action and perspectives

Orvosi Hetilap ◽

10.1556/oh.2009.28739 ◽

2009 ◽

Vol 150 (45) ◽

pp. 2051-2059 ◽

Cited By ~ 2

Author(s):

Miklós Tóth

Keyword(s):

Skeletal Muscle ◽

Androgen Receptor ◽

Conformational Changes ◽

Anabolic Steroids ◽

Target Tissue ◽

Androgenic Activity ◽

Selective Androgen Receptor Modulators ◽

Transcriptional Coregulators ◽

Tissue Selectivity ◽

Receptor Modulators

Interest in anabolic steroids has been renewed in the last decade with the discovery of tissue-selective androgen receptor modulators exhibiting high myotropic and small androgenic activity. An explanation put forward by us in 1982 for the mechanism of the preferential myotropic effect of nandrolone (19-nortestosterone) exploits the fundamental difference between the 5α-reductase concentrations in skeletal muscle and androgenic target tissue. In androgenic tissue, testosterone is converted to the more potent 5α-dihydrotestosterone whereas nandrolone is converted to a less potent derivative. As 5α-reduction is negligible in skeletal muscle, this explains why nandrolone shows a greater myotropic to androgenic ratio when compared with testosterone. Anabolic steroids that do not undergo 5α-reduction exert myotropic-androgenic dissociation because their effect in androgenic tissues is not amplified by 5α-reduction. Tissue selectivity by receptor modulators may be achieved by inducing specific conformational changes of the androgen receptor that affect its interaction with transcriptional coregulators. Anabolic activity is mediated by the stimulation of ribosomal RNA synthesis therefore regulation of this synthesis by anabolic steroids would deserve detailed studies.

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Comparative safety evaluation of selective androgen receptor modulators and anabolic androgenic steroids

Expert Opinion on Drug Safety ◽

10.1517/14740338.2015.1094052 ◽

2015 ◽

Vol 14 (11) ◽

pp. 1773-1785 ◽

Cited By ~ 24

Author(s):

Seul Min Choi ◽

Byung-Mu Lee

Keyword(s):

Androgen Receptor ◽

Safety Evaluation ◽

Anabolic Androgenic Steroids ◽

Selective Androgen Receptor Modulators ◽

Comparative Safety ◽

Androgenic Steroids ◽

Receptor Modulators

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SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARM) – A NEW TEMPTATION IN SPORTS. TYPES, MODE OF ACTION AND SIDE EFFECTS OF THEIR APPLICATION: REVIEW

Journal of Applied Sports Sciences ◽

10.37393/jass.2020.02.9 ◽

2020 ◽

Vol 2 (2020) ◽

pp. 107-115

Author(s):

Veselin Vasilev ◽

◽

Nikolay Boyadjiev ◽

Keyword(s):

Androgen Receptor ◽

Side Effects ◽

Androgen Receptors ◽

Target Cells ◽

Receptor Ligands ◽

Potential Health ◽

Adverse Side Effects ◽

Selective Androgen Receptor Modulators ◽

Androgenic Effect ◽

Receptor Modulators

ABSTRACT The selective androgen receptor modulators (SARMs) are androgen receptor ligands that bind to androgen receptors on target cells and exhibit a more pronounced anabolic effect at the expense of the androgenic effect on the latter. The aim of the article is to explain what SARMs are and how they are connected with sports. We used over 300 articles for the last 20 years connected with SARMs. Recently, the interest in these new molecules and their use has grown significantly, including in sports, which has led to their listing on the WADA prohibited list. In recent years, a lot of data have been gathered, both on the mechanism of action of a number of steroidal and non-steroidal representatives of this class of substances and on the adverse side effects of their use, as the latter should be well-known to sports doctors and especially to amateurs practicing in their free time and willing to increase their muscle mass with a view to preventing any potential health risks.

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Treatment of Hypogonadism: Current and Future Therapies

F1000Research ◽

10.12688/f1000research.10102.1 ◽

2017 ◽

Vol 6 ◽

pp. 68 ◽

Cited By ~ 7

Author(s):

Arthi Thirumalai ◽

Kathryn E. Berkseth ◽

John K. Amory

Keyword(s):

Androgen Receptor ◽

Side Effects ◽

Alternative Therapies ◽

Male Hypogonadism ◽

Selective Androgen Receptor Modulators ◽

The Future ◽

Patient Groups ◽

Receptor Modulators

The treatment of hypogonadism in men is of great interest to both patients and providers. There are a number of testosterone formulations currently available and several additional formulations under development. In addition, there are some lesser-used alternative therapies for the management of male hypogonadism, which may have advantages for certain patient groups. The future of hypogonadism therapy may lie in the development of selective androgen receptor modulators that allow the benefits of androgens whilst minimizing unwanted side effects.

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Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review

Steroids ◽

10.1016/j.steroids.2020.108753 ◽

2020 ◽

Vol 164 ◽

pp. 108753

Author(s):

Steven B. Machek ◽

Thomas D. Cardaci ◽

Dylan T. Wilburn ◽

Darryn S. Willoughby

Keyword(s):

Androgen Receptor ◽

Deleterious Effect ◽

Narrative Review ◽

Anabolic Androgenic Steroids ◽

Selective Androgen Receptor Modulators ◽

Androgenic Steroids ◽

Receptor Modulators

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Novel Protective Group Synthesis of Androgen Receptor Modulators with Steroidal and Nonsteroidal Scaffolds

10.26434/chemrxiv.11346962 ◽

2019 ◽

Author(s):

Matthias Grill ◽

Melanie Patt ◽

Alex Odermatt

Keyword(s):

Androgen Receptor ◽

Molecular Mechanisms ◽

Anabolic Androgenic Steroids ◽

Protective Group ◽

Mood Changes ◽

Selective Androgen Receptor Modulators ◽

And Performance ◽

Androgenic Steroids ◽

Receptor Modulators

Anabolic androgenic steroids (AAS) are frequently used either clinically, by athletes, or for body shaping due to their muscle building and performance enhancing properties. AAS misuse is associated with cardiovascular diseases, mood changes and endocrine issues. Despite the recognition of the severe adverse effects of AAS misuse, the underlying molecular mechanisms are insufficiently understood. Selective androgen receptor modulators (SARMs) are supposed to diminish the adverse androgenic AAS effects while maximizing anabolic effects. In order to obtain androgen receptor modulating compounds of high purity for mechanistic in vitro investigations, this study summarizes protocols of optimized chemical synthesis for five AAS and two SARMs.

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