In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls
| Deutscher übersetzter Titel: | In-vitro-Metabolismus von GW1516 und Implementierung seiner Hauptmetaboliten in die Routine-Dopingkontrollen |
|---|---|
| Autor: | Möller, Ines; Thomas, Andreas; Beuck, Simon; Rodchenkov, Grigory; Bornatsch, Wolfgang; Geyer, Hans; Schänzer, Wilhelm; Thevis, Mario |
| Erschienen in: | Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop ; 28th Cologne Workshop on Dope Analysis , 7th to 12th March 2010 |
| Veröffentlicht: | Köln: Sportverl. Strauß (Verlag), 2010, S. 17-26, Lit. |
| Format: | Literatur (SPOLIT) |
| Publikationstyp: | Sammelwerksbeitrag |
| Medienart: | Gedruckte Ressource |
| Sprache: | Englisch |
| Schlagworte: | |
| Online Zugang: | |
| Erfassungsnummer: | PU201108006606 |
| Quelle: | BISp |
Abstract
The PPARδ-agonist GW1516 is categorized as a gene doping substance by the World Anti-Doping Agency due to its upregulation of genes associated with oxidative metabolism and a modified substrate preference potentially resulting in an improved athletic performance. To enable the detection of abuse in sport via analysis of urine specimens, the phase-I and -II metabolism of GW1516 was simulated by an in-vitro assay. Two oxygenated metabolites (sulfoxide and sulfone) were identified as main phase-I metabolites as well as one hydroxylation and the respective monoglucuronides of GW1516 and the oxygenated metabolites as phase-II metabolites. As the sulfoxide and the sulfone were both excreted in urine, they were chosen as target analytes and successfully implemented in routine doping control procedures. Verf.-Referat