ChemInform Abstract: Nonsteroidal Selective Androgen Receptor Modulators (SARMs): Dissociating the Anabolic and Androgenic Activities of the Androgen Receptor for Therapeutic Benefit

Abstract

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In vitro Metabolism Studies on the Selective Androgen Receptor Modulator LG121071 and its Implementation into Human Doping Controls Using Liquid Chromatography-Mass Spectrometry

“…The induced anabolic effects support muscle growth and bone density as well as strength and physical fitness. These beneficial effects substantiate their potential for abuse in sports [2][3][4][5][6] and since 2008 SARMs have been prohibited according to the regulations of the World Anti-Doping Agency (WADA). 7 In 2010 the first SARM-positive doping control samples 8,9 corroborated former suspicions that arose from available black-market products.…”

“…Employing MS 3 experiments, the subsequent dissociation of m/z 269 to m/z 241 by eliminating another ethene unit (28 u) was shown ( Table 1). In consideration of the production mass spectrum of the deuterated analyte [ Figure 3(b)] and also the MS 3 and accurate mass data generated from m/z 272 (Table 1), the loss of C-12 and C-13 was suggested, yielding the tentatively assigned structure of protonated 7-imino-6-methylene-4-(trifluoromethyl)-6,7-dihydroquinolin-2(1H)-one for m/z 241, as illustrated in Figure 4. In the case of the isotope-labeled LG121071, differently deuterated species of the corresponding product ions were observed at m/z 241, 242 and 243, and are attributable to H/D randomization and rearrangement processes occurring with the neutral loss of ethane.…”