Magalhães, Wendell S. Garrido, Bruno C. Cavalcanti, Gustavo A. Padilha, Monica C. Casilli, Alessandro Pereira, Henrique M. G. Aquino Neto, Francisco R. de Human Metabolism of the Anabolic Steroid Methasterone: Detection and Kinetic Excretion of New Phase I Urinary Metabolites and Investigation of Phase II Metabolism by GC-MS and UPLC-MS/MS <div><p>Methasterone is a designer anabolic steroid that is prohibited for athletes and is monitored by anti-doping laboratories. In this work, our objective is to discover new human phase I metabolites, define their excretion kinetics for 30 days and analyze their phase II metabolism (sulfate, cysteine and N-acetylcysteine conjugates). Urine samples from four volunteers were analyzed by chromatographic techniques. Through gas chromatography coupled to mass spectrometry analysis it was possible to detect methasterone and its nine phase I metabolites in the urine samples after glucuronide enzymatic hydrolysis, from which one were previously unreported. These nine compounds were not excreted in free form. The new proposed metabolite is 17β-hydroxy-2α,17α-dimethyl-5β-androstan-3-one, obtained from the epimerization at C5. The 3α-hydroxy metabolite, currently monitored by anti-doping laboratories, was the most abundant and was detected for the longest time. Furthermore, four other long-term metabolites were identified. By ultra-performance liquid chromatography coupled to tandem mass spectrometry, only the drug and a known metabolite were detected after glucuronide hydrolysis, and phase II metabolites were not found. Thus, our results contribute to elucidating methasterone metabolism, including long-term metabolites besides of the 3α-hydroxy in routine doping analysis, which is very important due to variation in human metabolism.</p></div> methasterone;doping;human metabolism;gas chromatography;ultra-performance liquid chromatography 2019-05-29
    https://scielo.figshare.com/articles/dataset/Human_Metabolism_of_the_Anabolic_Steroid_Methasterone_Detection_and_Kinetic_Excretion_of_New_Phase_I_Urinary_Metabolites_and_Investigation_of_Phase_II_Metabolism_by_GC-MS_and_UPLC-MS_MS/8195078
10.6084/m9.figshare.8195078.v1