Nafoxidine
Nafoxidine is a nonsteroidal SERM that was previously under investigation for potential medical applications but was never marketed. It is structurally related to tamoxifen, another SERM that is widely used for the treatment of breast cancer.
Chemistry
Nafoxidine is a nonsteroidal compound, meaning it does not have a steroid backbone structure common to steroid hormones like estrogen. Instead, it has a phenyl group, a piperidine ring, and a naphthalene ring, which together form a unique structure that allows it to bind to estrogen receptors.
Pharmacology
Nafoxidine acts as a SERM, or selective estrogen receptor modulator. This means it can act as an agonist or antagonist of the estrogen receptor depending on the tissue type. In some tissues, such as the breast, it acts as an antagonist, blocking the effects of estrogen and potentially helping to prevent or treat estrogen-sensitive cancers. In other tissues, such as the bone and cardiovascular system, it acts as an agonist, mimicking the effects of estrogen and potentially providing beneficial effects.
Clinical Development
Nafoxidine was initially developed in the 1970s and underwent clinical trials for the treatment of breast cancer. However, it was found to cause cataracts in animal studies, which led to its development being discontinued. Despite this, it has been used in research settings to study the function of estrogen receptors and the effects of SERMs.
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