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In animal studies clenbuterol hydrochloride is shown to exhibit anabolic activity, obviously an attractive trait to a bodybuilder or athlete. It is also been used in the treatment of various inflammatory and autoimmune disorders. However, the effects of clenbuterol on muscle mass have not been fully elucidated. Chronically elevated clenbuterol levels have been detected among postmenopausal steroid users in various countries, such as Denmark, Greece, Norway, Switzerland, and the UK (see reference 1). There is evidence that the circulating concentration of glucuronidated clenbuterol is significantly reduced in postmenopausal steroid users (1, 3, 4). However, the effect is limited to a significant subgroup of these users and the results are inconclusive (5). An in vitro study showed that glucuronidated clenbuterol inhibits the activity of the mitogen-activated protein kinase system and the mitogenic factor 2, 3-kinase. No effect on the activity of the protein kinase cascade was observed in normal rats (4). However, in vitro studies showed that glucuronidated clenbuterol inhibited the cyclooxygenase-2 (1, 3, 4, 6) activity in rat muscle cells (7). Although the mechanisms governing the reduction in cyclooxygenase-2 activity in the rat are not known, it has recently been postulated that glucuronidated clenbuterol inhibits this enzyme (8). It is well known that clenbuterol has a strong antidiabetic activity, an antihyperglycemic agent, and a potential in vivo vasodilator as well (9). In contrast, this drug has adverse effects on bone marrow function and its use may be problematic for the athlete. As it is often not well tolerated in a clinical setting as is commonly seen with anabolic agents, it is not known to which extent clenbuterol use in a clinic setting might translate to the clinic. In one study, glucuronidated clenbuterol used by female steroid abusers without the use of hormonal therapy for 5–15 wk resulted in decreased bone mineral density in the hip and lower limb (10). Thus, while research on the antiandrogenic effects of clenbuterol does exist, to date, no studies have evaluated for the first time whether the antiandrogenic or the antihyperandrogenic effects of glucuronidated clenbuterol occur in normal male and female subjects. We believe that a prospective, controlled study is needed in the area of human health to investigate the effects of glucuronidated clenbuterol. Related Article: