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Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist–antagonist of the estrogen receptor (ER). [6] It has estrogenic effects in bone and antiestrogenic effects in the breasts and uterus. [6] Raloxifene was approved for medical use in the United States in 1997. [6] It is available as a generic medication.
When the interactive distance between raloxifene and Asp-351 is increased from 2.7 Å to 3.5-5 Å it causes increased estrogen-like action of the raloxifene-ERα complex. When the piperidine ring of raloxifene is replaced by cyclohexane, the ligand loses antiestrogenic properties and becomes a full agonist. The interaction between SERM's ...
Estradiol/raloxifene (E2/RLX) is a tissue-selective estrogen complex (TSEC) which was studied for potential use in menopausal hormone therapy but was never marketed. [ 2 ] [ 1 ] [ 3 ] [ 4 ] [ 5 ] Today, E2/RLX is not generally used due to concerns of endometrial hyperplasia .
Lasofoxifene, sold under the brand name Fablyn, is a nonsteroidal selective estrogen receptor modulator (SERM) which is marketed by Pfizer in Lithuania and Portugal for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy, [1] [2] and the result of an exclusive research collaboration with Ligand Pharmaceuticals (LGND).
Research from male rhesus monkeys suggests testosterone functions to increase sexual motivation, thereby motivating males to compete for access to sexual partners. It is postulated that the motivating effects of testosterone in male rhesus monkeys promotes successful sexual competition and may be particularly important motivating tools for low ...
In 1980, Jordan joined the University of Wisconsin–Madison where he started to look at the effects of tamoxifen and another SERM, raloxifene, on bone density and coronary systems. This was needed because of the concern that long term use of SERMs could lead to osteoporosis and heart disease. Jordan's research showed that post-menopausal women ...
Use of combined oral contraceptive pills, however, varies widely by country, [18] age, education, and marital status. For example, one third of women aged 16–49 in the United Kingdom use either the combined pill or progestogen-only pill (POP), [ 19 ] [ 20 ] compared with less than 3% of women in Japan (as of 1950–2014).
Development of the ring has led to several designs with different sizes, ring materials, and steroid formulations. Modern designs are made of plastic polymer rings containing sex steroids which diffuse out of the ring directly into the vaginal epithelium and into systemic circulation.