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Int. J. Mol. Sci. 2016, 17(10), 1676; doi:10.3390/ijms17101676

In Vitro Metabolic Studies of REV-ERB Agonists SR9009 and SR9011

Department of Clinical Chemistry, Microbiology and Immunology, Doping Control Laboratory (DoCoLab), Ghent University, Technologiepark 30 B, B-9052 Zwijnaarde, 9000 Ghent, Belgium
Author to whom correspondence should be addressed.
Academic Editor: Chang Won Choi
Received: 5 August 2016 / Revised: 21 September 2016 / Accepted: 26 September 2016 / Published: 3 October 2016
(This article belongs to the Section Molecular Pathology, Diagnostics, and Therapeutics)
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SR9009 and SR9011 are attractive as performance-enhancing substances due to their REV-ERB agonist effects and thus circadian rhythm modulation activity. Although no pharmaceutical preparations are available yet, illicit use of SR9009 and SR9011 for doping purposes can be anticipated, especially since SR9009 is marketed in illicit products. Therefore, the aim was to identify potential diagnostic metabolites via in vitro metabolic studies to ensure effective (doping) control. The presence of SR9009 could be demonstrated in a black market product purchased over the Internet. Via human liver microsomal metabolic assays, eight metabolites were detected for SR9009 and fourteen metabolites for SR9011 by liquid chromatography-high resolution mass spectrometry (LC–HRMS). Structure elucidation was performed for all metabolites by LC–HRMS product ion scans in both positive and negative ionization mode. Retrospective data analysis was applied to 1511 doping control samples previously analyzed by a full-scan LC–HRMS screening method to verify the presence of SR9009, SR9011 and their metabolites. So far, the presence of neither the parent compound nor the metabolites could be detected in routine urine samples. However, to further discourage use of these potentially harmful compounds, incorporation of SR9009 and SR9011 into screening methods is highly recommended. View Full-Text
Keywords: REV-ERB agonists; SR9009; SR9011; phase I metabolism; in vitro studies; liquid chromatography–high resolution mass spectrometry (LC–HRMS); doping agents REV-ERB agonists; SR9009; SR9011; phase I metabolism; in vitro studies; liquid chromatography–high resolution mass spectrometry (LC–HRMS); doping agents

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Geldof, L.; Deventer, K.; Roels, K.; Tudela, E.; Van Eeno, P. In Vitro Metabolic Studies of REV-ERB Agonists SR9009 and SR9011. Int. J. Mol. Sci. 2016, 17, 1676.

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