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Synthetic Anabolic Agents: Steroids and Nonsteroidal Selective Androgen Receptor Modulators

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Doping in Sports: Biochemical Principles, Effects and Analysis

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 195))

Abstract

The central role of testosterone in the development of male characteristics, as well as its beneficial effects on physical performance and muscle growth, has led to the search for synthetic alternatives with improved pharmacological profiles. Hundreds of steroidal analogs have been prepared with a superior oral bioavailability, which should also possess reduced undesirable effects. However, only a few entered the pharmaceutical market due to severe toxicological incidences that were mainly attributed to the lack of tissue selectivity. Prominent representatives of anabolic-androgenic steroids (AAS) are for instance methyltestosterone, metandienone and stanozolol, which are discussed as model compounds with regard to general pharmacological aspects of synthetic AAS. Recently, nonsteroidal alternatives to AAS have been developed that selectively activate the androgen receptor in either muscle tissue or bones. These so-called selective androgen receptor modulators (SARMs) are currently undergoing late clinical trials (IIb) and will be prohibited by the World Anti-Doping Agency from January 2008. Their entirely synthetic structures are barely related to steroids, but particular functional groups allow for the tissue-selective activation or inhibition of androgen receptors and, thus, the stimulation of muscle growth without the risk of severe undesirable effects commonly observed in steroid replacement therapies. Hence, these compounds possess a high potential for misuse in sports and will be the subject of future doping control assays.

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Acknowledgments

The authors thank the Ministry of the Interior of the Federal Republic of Germany and the Manfred-Donike Institute for Doping Analysis, Cologne, for their support.

Author information

Authors and Affiliations

  1. Center for Preventive Doping Research – Institute of Biochemistry, German Sport University Cologne, Am Sportpark Müngersdorf 6, 50933, Cologne, Germany

    Mario Thevis

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  1. Mario Thevis
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  2. Wilhelm Schänzer
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Correspondence to Mario Thevis .

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Editors and Affiliations

  1. Sportbiochemie Dresden, Institut für Dopinganalytik und, Dresdner Straße 12, Kreischa, 01731, Germany

    Detlef Thieme

  2. Gamle Trondheimsvei 39, Hagan, 1481, Norway

    Peter Hemmersbach

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Thevis, M., Schänzer, W. (2010). Synthetic Anabolic Agents: Steroids and Nonsteroidal Selective Androgen Receptor Modulators. In: Thieme, D., Hemmersbach, P. (eds) Doping in Sports: Biochemical Principles, Effects and Analysis. Handbook of Experimental Pharmacology, vol 195. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-79088-4_5

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