Tibolone is a synthetic steroid with progesterone-like activity. It binds to the progesterone receptor, which is primarily located in the uterus and ovaries. Tibolone has been shown to be an effective treatment for postmenopausal osteoporosis and may also have non-hormonal effects on the central nervous system, such as anti-depressant and anti-anxiety effects. Tibolone binds to the progesterone receptor through a stepwise process, binding more strongly than progesterone due to its substitution of a hydroxyl group at C4 for hydrogen. Tibolone has also been shown to be an effective overtraining prevention agent, by reducing the risk of neural injury during exercise. This drug can also be used as an effective treatment against depression, anxiety and overtraining syndrome.
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