Antileishmanial Activity of the Estrogen Receptor Modulator Raloxifene

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Antileishmanial Activity of the Estrogen Receptor Modulator Raloxifene

BACKGROUND The treatment of leishmaniasis relies mostly on parenteral drugs with potentially serious adverse effects. Additionally, parasite resistance in the treatment of leishmaniasis has been demonstrated for the majority of drugs available, making the search for more effective and less toxic drugs and treatment regimens a priority for the control of leishmaniasis. The aims of this study wer...

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Hypocholesterolemic 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...

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Inhibition of intimal hyperplasia using the selective estrogen receptor modulator raloxifene.

HYPOTHESIS The selective estrogen receptor modulator raloxifene hydrochloride inhibits intimal hyperplasia. DESIGN Controlled laboratory experiment. SETTING Experimental animal model. INTERVENTION AND MAIN OUTCOME MEASURES Forty-three senile female sheep were randomized to sham operation, ovariectomy, or ovariectomy followed by treatment with 17beta-estradiol or raloxifene. Six months aft...

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Nongenomic mechanisms of endothelial nitric oxide synthase activation by the selective estrogen receptor modulator raloxifene.

BACKGROUND Nontranscriptional signaling through estrogen receptors (ERs) is important in the cardiovascular system. In particular, estrogen stimulates endothelial NO synthase (eNOS) via the phosphatidylinositol 3-kinase (PI3K) pathway. The selective estrogen receptor modulator (SERM) raloxifene is effective for the treatment of postmenopausal osteoporosis, but its ability to activate eNOS via P...

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The Selective Estrogen Receptor Modulator Raloxifene Inhibits Neutrophil Extracellular Trap Formation

Raloxifene is a selective estrogen receptor modulator typically prescribed for the prevention/treatment of osteoporosis in postmenopausal women. Although raloxifene is known to have anti-inflammatory properties, its effects on human neutrophils, the primary phagocytic leukocytes of the immune system, remain poorly understood. Here, through a screen of pharmacologically active small molecules, w...

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ژورنال

عنوان ژورنال: PLoS Neglected Tropical Diseases

سال: 2014

ISSN: 1935-2735

DOI: 10.1371/journal.pntd.0002842