Epitestosterone has been identified for the natural ingredients of several mammals including human biological fluids. A long period of time, some people think this is a no hormone activity and metabolites, there is no any significant relationship between hormonal status in health and disease. Neither the biosynthetic pathway nor the site of its formation in man have been unequivocally confirmed to date. On one hand it apparently parallels the formation of testosterone, but on the other hand its concentration is not influenced by exogenous administration of testosterone. This fact creates the basis of the present doping control of testosterone abuse. In 1989 an observation was presented in a dermatological study that epitestosterone exerts an effect counteracting the action of testosterone on flank organ of Syrian hamster. Further studies showed that a complex action consisting of competitive binding of epitestosterone to androgen receptor, of inhibition of testosterone biosynthesis and its reduction to dihydrotestosterone and of antigonadotropic activity could be demonstrated in rat, mice and human tissues. It can be presumed that epitestosterone as a natural hormone can contribute to the regulation of such androgen dependent events as, e.g. the control of prostate growth or body hair distribution.
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