Universität zu Köln

Hansson, Annelie, Knych, Heather, Stanley, Scott, Thevis, Mario, Bondesson, Ulf and Hedeland, Mikael ORCID: 0000-0001-8962-2815 (2015). Characterization of equine urinary metabolites of selective androgen receptor modulators (SARMs) S1, S4 and S22 for doping control purposes. Drug Test. Anal., 7 (8). S. 673 - 684. HOBOKEN: WILEY-BLACKWELL. ISSN 1942-7611

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Abstract

Selective androgen receptor modulators, SARMs, constitute a class of compounds with anabolic properties but with few androgenic side-effects. This makes them possible substances of abuse and the World Anti-Doping Agency (WADA) has banned the entire class of substances. There have been several cases of illicit use of aryl propionamide SARMs in human sports and in 2013, 13 cases were reported. These substances have been found to be extensively metabolized in humans, making detection of metabolites necessary for doping control. SARMs are also of great interest to equine doping control, but the in vivo metabolite pattern and thus possible analytical targets have not been previously studied in this species. In this study, the urinary metabolites of the SARMs S1, S4, and S22 in horses were studied after intravenous injection, using ultra high performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UHPLC-QToF-MS). Eight different metabolites were found for SARM S1, nine for SARM S4, and seven for SARM S22. The equine urinary metabolite profiles differed significantly from those of humans. The parent compounds were only detected for SARMs S4 and S22 and only at the first sampling time point at 3h post administration, making them unsuitable as target compounds. For all three SARMs tested, the metabolite yielding the highest response had undergone amide hydrolysis, hydroxylation and sulfonation. The resulting phase II metabolites (4-nitro-3-trifluoro-methyl-phenylamine sulfate for SARMs S1 and S4 and 4-cyano-3-trifluoro-methyl-phenylamine sulfate for SARM S22) are proposed as analytical targets for use in equine doping control. Copyright (c) 2015 John Wiley & Sons, Ltd.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Hansson, Annelie UNSPECIFIED UNSPECIFIED UNSPECIFIED Knych, Heather UNSPECIFIED UNSPECIFIED UNSPECIFIED Stanley, Scott UNSPECIFIED UNSPECIFIED UNSPECIFIED Thevis, Mario UNSPECIFIED UNSPECIFIED UNSPECIFIED Bondesson, Ulf UNSPECIFIED UNSPECIFIED UNSPECIFIED Hedeland, Mikael UNSPECIFIED orcid.org/0000-0001-8962-2815 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-397445
DOI:	10.1002/dta.1768
Journal or Publication Title:	Drug Test. Anal.
Volume:	7
Number:	8
Page Range:	S. 673 - 684
Date:	2015
Publisher:	WILEY-BLACKWELL
Place of Publication:	HOBOKEN
ISSN:	1942-7611
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language MASS-SPECTROMETRIC CHARACTERIZATION; IN-VITRO; S-4 ANDARINE Multiple languages Biochemical Research Methods; Chemistry, Analytical; Pharmacology & Pharmacy Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/39744