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Characterization of...
Characterization of a non-approved selective androgen receptor modulator drug candidate sold via the Internet and identification of in vitro generated phase-I metabolites for human sports drug testing
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Thevis, Mario (författare)
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Lagojda, Andreas (författare)
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Kuehne, Dirk (författare)
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Thomas, Andreas (författare)
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Dib, Josef (författare)
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- Hansson, Annelie (författare)
- Uppsala universitet,Avdelningen för analytisk farmaceutisk kemi
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- Hedeland, Mikael (författare)
- Uppsala universitet,Avdelningen för analytisk farmaceutisk kemi
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- Bondesson, Ulf (författare)
- Uppsala universitet,Avdelningen för analytisk farmaceutisk kemi
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Wigger, Tina (författare)
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Karst, Uwe (författare)
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Schaenzer, Wilhelm (författare)
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(creator_code:org_t)
- 2015-04-22
- 2015
- Engelska.
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Ingår i: Rapid Communications in Mass Spectrometry. - : Wiley. - 0951-4198 .- 1097-0231. ; 29:11, s. 991-999
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- RATIONALE: Potentially performance-enhancing agents, particularly anabolic agents, are advertised and distributed by Internet-based suppliers to a substantial extent. Among these anabolic agents, a substance referred to as LGD-4033 has been made available, comprising the core structure of a class of selective androgen receptor modulators (SARMs). METHODS: In order to provide comprehensive analytical data for doping controls, the substance was obtained and characterized by nuclear magnetic resonance spectroscopy (NMR) and liquid chromatography/electrospray ionization high resolution/high accuracy tandem mass spectrometry (LC/ESI-HRMS). Following the identification of 4-(2-(2,2,2-trifluoro-1-hydroxyethyl) pyrrolidin-1-yl)-2-(trifluoromethyl) benzonitrile, the substance was subjected to in vitro metabolism studies employing human liver microsomes and Cunninghamella elegans (C. elegans) preparations as well as electrochemical metabolism simulations. RESULTS: By means of LC/ESI-HRMS, five main phase-I metabolites were identified as products of liver microsomal preparations including three monohydroxylated and two bishydroxylated species. The two most abundant metabolites (one mono-and one bishydroxylated product) were structurally confirmed by LC/ESI-HRMS and NMR. Comparing the metabolic conversion of 4-(2-(2,2,2-trifluoro-1-hydroxyethyl) pyrrolidin-1-yl)-2-(trifluoromethyl) benzonitrile observed in human liver microsomes with C. elegans and electrochemically derived metabolites, one monohydroxylated product was found to be predominantly formed in all three methodologies. CONCLUSIONS: The implementation of the intact SARM-like compound and its presumed urinary phase-I metabolites into routine doping controls is suggested to expand and complement existing sports drug testing methods.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
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Thevis, Mario
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Lagojda, Andreas
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Kuehne, Dirk
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Thomas, Andreas
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Dib, Josef
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Hansson, Annelie
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visa fler...
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Hedeland, Mikael
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Bondesson, Ulf
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Wigger, Tina
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Karst, Uwe
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Schaenzer, Wilhe ...
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visa färre...
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Uppsala universitet