Metabolic studies of 1-testosterone in horses.
Abstract: 1-Testosterone (17β-hydroxy-5α-androst-1-en-3-one), a synthetic anabolic steroid, has been described as one of the most effective muscle-building supplements currently on the market. It has an anabolic potency of 200 as compared to 26 for testosterone. Apart from its abuse in human sports, it can also be a doping agent in racehorses. Metabolic studies on 1-testosterone have only been reported for human in the early seventies, whereas little is known about its metabolic fate in horses. This paper describes the studies of in vitro and in vivo metabolism of 1-testosterone in horses, with the aim of identifying the most appropriate target metabolites to be monitored for controlling the misuse or abuse of 1-testosterone in racehorses. Six in vitro metabolites, namely 5α-androst-1-ene-3α,17β-diol (T1a), 5α-androstane-3β,17β-diol (T2), epiandrosterone (T3), 16,17-dihydroxy-5α-androst-1-ene-3-one (T4 & T5), and 5α-androst-1-ene-3,17-dione (T6), were identified. For the in vivo studies, two thoroughbred geldings were each administered orally with 800 mg of 1-testosterone by stomach tubing. The results revealed that the parent drug and eight metabolites were detected in urine. Besides the four in vitro metabolites (T1a, T2, T3, and T5), four other urinary metabolites, namely 5α-androst-1-ene-3β,17α-diol (T1b), 5α-androst-1-ene-3β,17β-diol (T1c), 5α-androstane-3α,17α-diol (T7) and 5α-androstane-3β,17α-diol (T8) were identified. This study shows that the detection of 1-testosterone administration is best achieved by monitoring the parent drug, which could be detected for up to 30 h post-administration.
Copyright © 2012 John Wiley & Sons, Ltd.
Publication Date: 2012-06-20 PubMed ID: 22715048DOI: 10.1002/dta.1380Google Scholar: Lookup
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Summary
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The research is focused on studying the metabolic impact of 1-Testosterone, a potent synthetic muscle-building supplement, on horses. It aims to understand its metabolic fate in horses in order to control its misuse in racing horses by monitoring specific target metabolites.
Understanding the Impact of 1-Testosterone in Horses
- This paper expands on the limited understanding of how 1-testosterone, an anabolic steroid with significant muscle-building properties, is metabolised in horses. While its metabolic pathways are somewhat known in humans, there is scarce information available for horses.
- The anabolic potency of 1-testosterone is approximately 200, which is quite high when compared to regular testosterone, which has an anabolic potency of 26. This makes 1-testosterone a powerful compound for increasing muscle mass.
- There are concerns regarding the abuse of 1-testosterone in horse racing because of its potential to significantly enhance performance, and thus this research is aimed towards identifying best practices for curbing such misuse.
In-Vitro and In-Vivo Metabolic Studies of 1-Testosterone in Horses
- In-vitro metabolic studies identified six metabolites, while in-vivo studies on two Thoroughbred geldings identified the parent drug and eight metabolites in urine samples post-administration of 1-Testosterone.
- These in-vitro and in-vivo studies provide potential pathways for tracking the presence of 1-testosterone in the body by focusing on particular target metabolites.
- The identified metabolites can serve as biomarkers, providing an opportunity to determine the presence of 1-testosterone in the system through simple urine tests. This could lead to developing robust doping controls in horse racing.
Detecting 1-Testosterone in Horses
- The research concludes that the most effective way to track 1-testosterone administration in horses is by monitoring the parent drug. This method allows for the detection of 1-testosterone up to 30 hours post-administration.
- By focusing on the parent drug rather than its metabolites, it is possible to achieve a more straightforward and effective approach to monitoring and controlling the abuse of 1-testosterone in the racehorse industry.
Cite This Article
APA
Kwok WH, Ho EN, Leung GN, Tang FP, Wan TS, Wong HN, Yeung JH.
(2012).
Metabolic studies of 1-testosterone in horses.
Drug Test Anal, 5(2), 81-88.
https://doi.org/10.1002/dta.1380 Publication
Researcher Affiliations
- Racing Laboratory, The Hong Kong Jockey Club, Sha Tin Racecourse, Sha Tin, N.T., Hong Kong, China.
MeSH Terms
- Anabolic Agents / metabolism
- Anabolic Agents / urine
- Animals
- Gas Chromatography-Mass Spectrometry
- Horses / metabolism
- Horses / urine
- Microsomes, Liver / metabolism
- Testosterone / analogs & derivatives
- Testosterone / metabolism
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