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Characterization of...
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Thevis, Mario
(författare)
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
- Artikel/kapitelEngelska2015
Förlag, utgivningsår, omfång ...
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2015-04-22
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Wiley,2015
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printrdacarrier
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LIBRIS-ID:oai:DiVA.org:uu-256112
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https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-256112URI
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https://doi.org/10.1002/rcm.7189DOI
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Språk:engelska
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Sammanfattning på:engelska
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Ämneskategori:ref swepub-contenttype
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Ämneskategori:art swepub-publicationtype
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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.
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Biuppslag (personer, institutioner, konferenser, titlar ...)
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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, AnnelieUppsala universitet,Avdelningen för analytisk farmaceutisk kemi(Swepub:uu)annha905
(författare)
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Hedeland, MikaelUppsala universitet,Avdelningen för analytisk farmaceutisk kemi(Swepub:uu)mikahede
(författare)
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Bondesson, UlfUppsala universitet,Avdelningen för analytisk farmaceutisk kemi(Swepub:uu)ulfbonde
(författare)
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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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Uppsala universitetAvdelningen för analytisk farmaceutisk kemi
(creator_code:org_t)
Sammanhörande titlar
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Ingår i:Rapid Communications in Mass Spectrometry: Wiley29:11, s. 991-9990951-41981097-0231
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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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