Yale researchers create topical estrogen that alleviates sexual dysfunction in menopausal women and eliminates side effects of conventiona...( am Hochberg said. Since topica...),Health

"Since topically applied estrogen is absorbed into the blood, its purpose is defeated," Hochberg added. "A potent estrogen whose range is limited to the tissue to which it is applied is ideal for the treatment of menopausal disorders."

Using a derivative of estradiol, the major estrogen, that, because of its charge, was no longer estrogenic, Hochberg and his team masked this group-derivative by another substitution, resulting in a compound that was highly estrogenic, meaning it could bind the estrogen receptor protein that mediates the action of estrogen.

"This compound had high estrogenic potential and at the same time, it was designed to be metabolically labile, so it could be metabolized by an enzyme called esterase that converts this compound very rapidly back to the inactive parent," Hochberg said. "The consequence is that the estrogen could be metabolized extremely quickly in the bloodstream. Tests in female rats showed that there was very little systemic activity."

Hochberg and his team then tested the estrogen for vaginal activity. "We placed the material directly into the vaginas of mice where it was extremely estrogenic," he said. "In this test, we measured the production of a protein that is a marker for estrogen simulation of vaginal growth."

The new topical estrogen also includes anti-aging properties. Hochberg said that because the skin contains estrogen receptors, it is an estrogen target organ that can respond to estrogen replacement. "This new topical estrogen has some anti-aging properties and may alleviate some of the symptoms of aging skin," he said.

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Contact: Karen N. Peart
karen.peart@yale.edu
203-432-1326
Yale University
9-May-2001