New long ‐standing metabolites of 17α‐methyltestosterone are detected in HepG2 cell in vitro metabolic model and in human urine

Novel fully A-ring-reduced metabolites of methyltestosterone were predicted and synthesized on a microscale. Their GC-MS/(MS) behavior was studied to develop a targeted detection method. Targeted analysis of methyltestosterone HepG2 cell incubation supernatants and post-administration urine samples confirmed the presence of these novel methyltestosterone metabolites in both matrices. Evaluation of their human urine post-administration excretion profiles revealed that some of them could be used as additional long-term metabolites for the monitoring of methyltestosterone in the frame of doping control. AbstractNovel metabolites of the anabolic androgenic steroid 17 α-methyltestosterone have been detected in HepG2 cell in vitro metabolic model and in human urine. Their detection was accomplished through targeted gas chromatography–(tandem) mass spectrometry analysis that has been based on microscale synthesized standards. The related synthesis and the gas ch romatography–(tandem) mass spectrometry characterization of the analytical standards are described. All newly presented metabolites have a fully reduced steroid A-ring with either an 17,17-dimethyl-18-nor-Δ13 structure or they have been further oxidized at position 16 of the steroid backbone. Met abolites with 17,17-dimethyl-18-nor-Δ13 structure may be considered as side products of phase II metabolic sulfation of the 17β-hydroxy group of methyltestosterone or its reduced tetrahydro-methyltestosterone metabolites 17...
Source: Drug Testing and Analysis - Category: Drugs & Pharmacology Authors: Tags: RESEARCH ARTICLE Source Type: research