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Tetrahydrogestrinone Is a Potent Androgen and Progestin

Heart Research Institute (A.K.D.), Camperdown, Sydney, New South Wales 2050, Australia; University of Sydney (A.K.D., K.C.Y.M., D.J.H.), Sydney, New South Wales 2006, Australia; Australian Sports Drug Testing Laboratory (R.K.), Australian Government Analytical Laboratories, Pymble, New South Wales 2073, Australia; and ANZAC Research Institute (D.J.H.), Sydney, New South Wales 2139, Australia

Address all correspondence and requests for reprints to: Professor D. J. Handelsman, ANZAC Research Institute, Sydney, New South Wales 2139, Australia. E-mail: djh{at}anzac.edu.au.

Abstract

Tetrahydrogestrinone (THG) was recently identified as a novel steroid used illicitly to improve athletic performance. Although its structure is closely related to gestrinone, a 19-nor progestin, and resembles that of trenbolone, THG was never marketed, so information on its hormonal properties is not known. In this study, we demonstrate that THG is a highly potent androgen and progestin in a yeast-based in vitro bioassay system expressing human androgen and progesterone receptors. It has no estrogenic activity and no antagonism for any of the three steroid receptor classes.

Footnotes

Abbreviations: AR, Androgen receptor; ER, estrogen receptor; PR, progesterone receptor; THG, tetrahydrogestrinone.

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