Study summary · research use only
In Vitro Metabolism and Analytical Characterization of SLU-PP-332 and SLU-PP-915: Novel Pan-ERR Agonists With Doping Potential
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
This in vitro study (human liver S9 fraction and human liver microsomes) characterized SLU-PP-332 and SLU-PP-915, two pan-ERR agonists under investigation as exercise mimetics, using LC-HRMS/MS, with selected SLU-PP-915 metabolites also synthesized and analyzed by NMR. Nine metabolites were identified for SLU-PP-332, consisting of six Phase-I metabolites and three Phase-II conjugates. SLU-PP-915 yielded seven Phase-I transformation products, with three metabolites confirmed by chemical synthesis and NMR. The authors describe the findings as providing structural detail on the metabolism of these compounds, intended to support detection of their potential use as performance-enhancing substances in sports drug testing.
Abstract
Estrogen-related receptor (ERR) agonists such as the drug candidates SLU-PP-332 and SLU-PP-915 are currently being investigated as exercise mimetics, given their ability to trigger human physiological processes similar to those initiated by actual physical activity. This capability prompted the consideration of these compounds as drugs potentially relevant for sports drug testing programs. The two pan-ERR agonists SLU-PP-332 and SLU-PP-915 were characterized using liquid chromatography-high resolution (tandem) mass spectrometry (LC-HRMS/MS). Furthermore, the in vitro metabolic transformation products of both compounds prepared by means of human liver S9 fraction (S9 fraction) and human liver microsomes (HLMs) were analyzed. In addition, selected metabolites of SLU-PP-915 were synthesized and their structures were analyzed by nuclear magnetic resonance (NMR) spectroscopy. A total of nine metabolites were identified for SLU-PP-332, consisting of six Phase-I metabolites and three Phase-II conjugates. Conversely, the analysis of SLU-PP-915 yielded only Phase-I transformation products, with a total of seven metabolites identified. In both cases, an in-depth structural elucidation was conducted to obtain a comprehensive overview of the detected metabolites. Furthermore, three metabolites of SLU-PP-915 were confirmed through chemical synthesis and NMR. The results obtained in this study gave an in-depth view into the analysis and in vitro metabolism of the newly developed pan-ERR agonists SLU-PP-332 and SLU-PP-915. This may help to uncover the illicit use of these novel compounds as potential performance-enhancing substances.
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