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Biochemical and Physiological Aspects of Endogenous Androgens

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

Abstract

This review attempts to give a synopsis of the major aspects concerning the biochemistry of endogenous androgens, supplemented with several facets of physiology, particularly with respect to testosterone. Testosterone continues to be the most common adverse finding declared by World Anti-Doping Agency accredited laboratories, such samples having an augmented testosterone to epitestosterone ratio. Knowledge regarding the precursors and metabolism of endogenous testosterone is therefore fundamental to understanding many of the issues concerning doping with testosterone and its prohormones, including the detection of their administration. Further, adverse findings for nandrolone are frequent, but this steroid and 19-norandrostenedione are also produced endogenously, an appealing hypothesis being that they are minor by-products of the aromatization of androgens. At sports tribunals pertaining to adverse analytical findings of natural androgen administration, experts often raise issues that concern some aspect of steroid biochemistry and physiology. Salient topics included within this review are the origins and interconversion of endogenous androgens, the biosynthesis of testosterone and epitestosterone, the mechanism of aromatization, the molecular biology of the androgen receptor, the hypothalamic–pituitary–testicular axis, disturbances to this axis by anabolic steroid administration, the transport (binding) of androgens in blood, and briefly the metabolism and excretion of androgens.

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Acknowledgements

The author is very grateful to the following for helpful discussion: John Hackett, Assistant Professor in the Department of Medicinal Chemistry & Institute for Structural Biology and Drug Discovery of the Virginia Commonwealth University Medical Center, with regards to the aromatization mechanism and the possibility of nandrolone formation; Anita Payne, Professor of Obstetrics and Gynecology, Stanford University, with respect to the biosynthetic route of testosterone; and Professor Vivian James of Imperial College London, for his supportive comments.

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Kicman, A.T. (2010). Biochemical and Physiological Aspects of Endogenous Androgens. 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_2

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