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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.
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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 ...
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