title: Advantages and Limitations of Androgen Receptor-Based Methods for Detecting Anabolic Androgenic Steroid Abuse as Performance Enhancing Drugs.
abstract: Testosterone (T) and related androgens are performance enhancing drugs (PEDs) abused by some athletes to gain competitive advantage. To monitor unauthorized androgen abuse, doping control programs use mass spectrometry (MS) to detect androgens, synthetic anabolic-androgenic steroids (AASs) and their metabolites in an athlete's urine. AASs of unknown composition will not be detected by these procedures. Since AASs achieve their anabolic effects by activating the Androgen Receptor (AR), cell-based bioassays that measure the effect of a urine sample on AR activity are under investigation as complementary, pan-androgen detection methods. We evaluated an AR BioAssay as a monitor for androgen activity in urine pre-treated with glucuronidase, which releases T from the inactive T-glucuronide that predominates in urine. AR BioAssay activity levels were expressed as 'T-equivalent' concentrations by comparison to a T dose response curve. The T-equivalent concentrations of androgens in the urine of hypogonadal participants supplemented with T (in whom all androgenic activity should arise from T) were quantitatively identical to the T measurements conducted by MS at the UCLA Olympic Analytical Laboratory (0.96 ± 0.22). All 17 AASs studied were active in the AR BioAssay; other steroids were inactive. 12 metabolites of 10 commonly abused AASs, which are used for MS monitoring of AAS doping because of their prolonged presence in urine, had reduced or no AR BioAssay activity. Thus, the AR BioAssay can accurately and inexpensively monitor T, but its ability to monitor urinary AASs will be limited to a period immediately following doping in which the active AASs remain intact.
authors.affiliation: Center for Reproductive Sciences, University of California San Francisco, San Francisco, California, United States of America.
authors.forename: Kathy
authors.initials: K
authors.lastname: Bailey
authors.affiliation: Center for Reproductive Sciences, University of California San Francisco, San Francisco, California, United States of America.
authors.forename: Tahmineh
authors.initials: T
authors.lastname: Yazdi
authors.affiliation: Division of Endocrinology, University of California San Francisco, San Francisco, California, United States of America.
authors.forename: Umesh
authors.initials: U
authors.lastname: Masharani
authors.affiliation: Division of Endocrinology, University of California San Francisco, San Francisco, California, United States of America.
authors.forename: Blake
authors.initials: B
authors.lastname: Tyrrell
authors.affiliation: Department of Pathology and Laboratory Medicine, Geffen School of Medicine at UCLA, Los Angeles, California, United States of America.
authors.forename: Anthony
authors.initials: A
authors.lastname: Butch
authors.affiliation: Center for Reproductive Sciences, University of California San Francisco, San Francisco, California, United States of America.|Department of Obstetrics and Gynecology, University of California San Francisco, San Francisco, California, United States of America.
authors.forename: Fred
authors.initials: F
authors.lastname: Schaufele
mesh_terms: D045930:Anabolic Agents / Q000652:urine*; D000728:Androgens / Q000652:urine*; D001681:Biological Assay; D006801:Humans; D013058:Mass Spectrometry; D058573:Performance-Enhancing Substances / Q000652:urine*; D011944:Receptors, Androgen / Q000378:metabolism*; D013256:Steroids / Q000652:urine*; D015813:Substance Abuse Detection / Q000379:methods*; D013739:Testosterone / Q000652:urine
chemical_list: D045930:Anabolic Agents; D000728:Androgens; D058573:Performance-Enhancing Substances; D011944:Receptors, Androgen; D013256:Steroids; D013739:Testosterone