Characterization of growth hormone secretagogue small molecule ibutamoren (MK-0677) and its possible metabolites in thoroughbred horses for doping control.
Abstract: It is important to remember that performance-enhancing agents such as non-peptide growth hormone secretagogues present a significant risk of abuse. Ibutamoren (MK-0677) is a potent, long-acting, selective non-peptide growth hormone secretagogue that can be taken orally. Methods: This study examines ibutamoren and its metabolites in thoroughbred horses after oral administration. Liquid chromatography/high-resolution mass spectrometry was used to determine the probable structures of the detected metabolites. Results: In this study, 22 metabolites of ibutamoren were identified (17 phase I and 5 phase II). Oxidation of ibutamoren leads to hydroxylated metabolites (mono and di). The study also detected dissociated side chains (benzyl group and 2-amino-2-methylpropanamide) and hydrogenated metabolites. The glucuronic acid conjugated analogs of ibutamoren were detected during phase II of the study, but no sulfonic acid conjugated analogs were observed. The major metabolites can be detected up to 96 hours after a single dose, and ibutamoren can persist for up to 72 hours. Conclusions: These findings will aid in the detection of ibutamoren and the detection of its illegal use in competitive sports.
© 2022 John Wiley & Sons Ltd.
Publication Date: 2022-06-19 PubMed ID: 35716382DOI: 10.1002/rcm.9337Google Scholar: Lookup
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- Journal Article
Summary
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This research article discusses the characterization of the non-peptide growth hormone secretagogue ibutamoren (MK-0677) and its metabolites in thoroughbred horses to detect any illegal usage of it for enhancing performance.
Methods
- The article uses liquid chromatography and high-resolution mass spectrometry to study the structure of metabolites after orally administering ibutamoren to thoroughbred horses.
Results
- The researchers were able to identify 22 metabolites of ibutamoren, which includes 17 phase I metabolites and 5 phase II metabolites.
- Through their analysis, the researchers found that oxidation of ibutamoren leads to the creation of hydroxylated metabolites, either mono or di.
- They also found dissociated side chains in the form of benzyl group and 2-amino-2-methylpropanamide, as well as hydrogenated metabolites.
- During phase II of the research, they detected the glucuronic acid conjugated analogs of ibutamoren, however, no sulfonic acid conjugated analogs were observed.
- The research showed that major metabolites can be detected for up to 96 hours, while ibutamoren can persist for up to 72 hours.
Conclusions
- The findings in the study will be immensely beneficial for detecting the illegal use of ibutamoren in sports.
- These insights will help to establish reliable anti-doping control, maintaining the spirit of fair competition in sports events involving thoroughbred horses.
Cite This Article
APA
Philip M, Karakka Kal AK, Subhahar MB, Karatt TK, Mathew B, Koshy SA.
(2022).
Characterization of growth hormone secretagogue small molecule ibutamoren (MK-0677) and its possible metabolites in thoroughbred horses for doping control.
Rapid Commun Mass Spectrom, 36(18), e9337.
https://doi.org/10.1002/rcm.9337 Publication
Researcher Affiliations
- Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates.
- Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates.
- Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates.
- Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates.
- Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates.
- Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates.
MeSH Terms
- Animals
- Doping in Sports / prevention & control
- Growth Hormone
- Horses
- Indoles
- Secretagogues
- Spiro Compounds
- Substance Abuse Detection / methods
- Substance Abuse Detection / veterinary
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