Unravelling androgens in sport: Altrenogest shows strong activation of the androgen receptor in a mammalian cell bioassay.
Abstract: Altrenogest is a commonly used progestogen for the suppression of oestrus and associated distracting behaviours that interfere with training and performance of female racehorses. The steroid is derived from 19-nor testosterone and is structurally similar to the anabolic androgenic steroid, trenbolone. In this study, the relative androgen potency of altrenogest was determined by a kidney (HEK293) cell androgen bioassay. The HEK293 bioassay shows that in its pure form, altrenogest has a high relative potency compared with testosterone but is not as strong as β-trenbolone. Our results also show that altrenogest is able to activate the androgen receptor at the concentrations relevant to the administration regime of racehorses and retains its activity ex vivo. Thus, we show unequivocally that altrenogest, a progestogen used widely in female racehorses, acts as a strong androgen in a mammalian cell bioassay.
© 2020 John Wiley & Sons, Ltd.
Publication Date: 2020-10-26 PubMed ID: 33037724DOI: 10.1002/dta.2941Google Scholar: Lookup
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Summary
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The study investigates the androgen potency of altrenogest, a steroid used in female racehorses. The findings reveal that altrenogest demonstrates high relative potency as compared to testosterone, and can activate the androgen receptor in relevant concentrations, thus suggesting that it functions as a strong androgen.
Background
- This research study revolves around the understanding of the androgen potency of altrenogest, which is a progestogen in wide use in the racehorse industry. Altrenogest is used for suppressing oestrus and associated behaviours that may interfere with the training and performance of female racehorses. It is important to note that this compound is derived from 19-nor testosterone and closely resembles the structure of an anabolic androgenic steroid, trenbolone.
Methods and Findings
- The study used a kidney cell androgen bioassay (HEK293) to evaluate the relative androgen potency of altrenogest.
- The results of the HEK293 bioassay elucidated that pure form altrenogest demonstrated a high relative potency when compared with testosterone. However, it was found to not be as potent as β-trenbolone.
- The research further demonstrated that altrenogest could activate the androgen receptor at concentrations relevant to the administration regime of racehorses and that it retained its activity ex vivo.
Implications
- The study conclusively establishes that altrenogest, despite its primary use as a progestogen, acts as a strong androgen in a mammalian cell bioassay.
- This points towards the need for further study and regulation of the use of such substances, due to their significant impact on the physiological processes and performance of racehorses.
Cite This Article
APA
Gillon A, Ho ENM, Chan GHM, Kauff A, Hughes G, Lund RA, Ashley Z, Wan TSM, Heather AK.
(2020).
Unravelling androgens in sport: Altrenogest shows strong activation of the androgen receptor in a mammalian cell bioassay.
Drug Test Anal, 13(3), 523-528.
https://doi.org/10.1002/dta.2941 Publication
Researcher Affiliations
- Department of Physiology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
- Racing Laboratory, The Hong Kong Jockey Club, Sha Tin Racecourse, Sha Tin, N.T., Hong Kong, China.
- Racing Laboratory, The Hong Kong Jockey Club, Sha Tin Racecourse, Sha Tin, N.T., Hong Kong, China.
- Department of Physiology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
- Department of Physiology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
- Department of Physiology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
- Department of Physiology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
- Racing Laboratory, The Hong Kong Jockey Club, Sha Tin Racecourse, Sha Tin, N.T., Hong Kong, China.
- Department of Physiology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
MeSH Terms
- Androgens / pharmacology
- Animals
- Doping in Sports
- Female
- HEK293 Cells
- Horses
- Humans
- Male
- Progestins / pharmacology
- Trenbolone Acetate / analogs & derivatives
- Trenbolone Acetate / pharmacology
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