Estrogen receptor α-mediated adiposity-lowering and hypocholesterolemic actions of the selective estrogen receptor modulator acolbifene
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چکیده
منابع مشابه
Bioactivation of the selective estrogen receptor modulator acolbifene to quinone methides.
Although approved for the treatment of hormone-dependent breast cancer as well as for the prevention of breast cancer in high-risk women, the selective estrogen receptor modulator (SERM) tamoxifen has been associated with an increased risk of endometrial cancer in women. With an understanding of the potential carcinogenic mechanisms of these compounds, SERMs could in principle be designed or se...
متن کاملHypocholesterolemic activity of raloxifene (LY139481): pharmacological characterization as a selective estrogen receptor modulator.
After once-daily oral dosing in ovariectomized rats, raloxifene (LY139481) hydrochloride produced dose- and time-dependent reductions in serum cholesterol and high-density lipoprotein-cholesterol. Paired-feeding studies demonstrated that effects of raloxifene on serum lipids were not secondary to effects on food consumption. Maximal reductions in serum cholesterol occurred within 4 days of ralo...
متن کاملAntagonists Selective for Estrogen Receptor α.
To develop compounds that are antagonists on ER , but not ER , we have added basic side-chains typically found in nonsteroidal antiestrogens to pyrazole compounds that bind with much higher affinity to ER than to ER . In this way we have developed basic side-chain pyrazoles (BSC-pyrazoles) that are high affinity, potent, selective antagonists on ER . These BSCpyrazoles are themselves inactive o...
متن کاملReceptor in Breast Cancer Cells Expressing Wild-Type Estrogen -Selective Estrogen Receptor Modulator Complex α Receptor Gene Expression Profiles with Activation of the Estrogen
Selective Estrogen Receptor Modulators (SERMs) are a new class of drugs that bind to estrogen receptor (ER) and elicit agonistic or antagonistic responses, depending on the target tissue. We have developed an in vitro system in which some SERMs (4-hydroxytamoxifen and resveratrol) demonstrate estrogenic response through wild-type (wt) ER, whereas others (raloxifene and GW7604) remain antiestrog...
متن کاملThe selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats.
The cancer-preventing selective estrogen receptor modulator (SERM) acolbifene (ACOL) exerts a potent and pure antiestrogenic action in the mammary gland and uterus, yet it displays beneficial, estrogen-like actions on energy and lipid metabolism in rodents. The compound reduces food intake and strongly decreases cholesterolemia in rats fed a cholesterol-free diet. This study was designed to est...
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ژورنال
عنوان ژورنال: International Journal of Obesity
سال: 2005
ISSN: 0307-0565,1476-5497
DOI: 10.1038/sj.ijo.0803014