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Fluoxymesterone
Fluoxymesterone (trade name Halotestin) is an anabolic steroid with strong androgenic properties that has been used in the treatment of male hypogonadism, delayed puberty in males, and in the treatment of breast neoplasms in women. It is approximately 5 times as potent as testosterone.〔Dr. K.V. Sastry (2008). ''Endocrinology and Reproductive Biology''. Page 150. ISBN 81-7133-777-5.〕 The antitumor activity of fluoxymesterone appears related to reduction or competitive inhibition of prolactin receptors or estrogen receptors or production. Dissimilar to testosterone, halotestin has a 100% bioavailability, as the methylation of the 17''α''-position in halotestin inhibits hepatic metabolism by enzymatic oxidation of 17''β''-hydroxyl, allowing its absorption into the bloodstream for transport around the body. Whilst there are many legitimate pharmaceutical applications of halotestin, abuse of such anabolic
steroids is detrimental to professional athleticism; leading to the development of analytical techniques by which halotestin doping can be identified.
Like many C-17 alpha alkylated steroids, fluoxymesterone has poor binding to the androgen receptor. Even so, its actions are mediated by the androgen receptor, most-likely due to its prolonged plasma half-life which is approximately 9.2 hours.〔Seth Roberts (2009). ''Anabolic Pharmacology''.〕
==Analytical testing for steroid abuse in professional athletics==
Detection of halotestin and other such illegal anabolic steroids in sports is achieved by GS-MS identification of urinary excreted anabolic steroids and their metabolites. In a test for halotestin, a dry residue obtained from a urine sample is dissolved in dimethylformamide and a sulfur trioxide-pyridine complex and is heated with 1% potassium carbonate solution. Halotestin and many of its metabolites contain two polar hydroxyl groups, leading to intermolecular hydrogen bonding that increases their boiling point and reduces volatility. In order to attain a gaseous sample for GC-MS, the products of hydrolysis are extracted, dissolved in methanol and derivatised to form volatile trimethylsilyl (TMS) esters by adding ''N''-methyl-''N''-trimethylsilyl-trifluoroacetamide (MSTFA) and trimethylsilylimidazole (TMSImi).
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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