Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats.

摘要: For the first time, four well-characterized compounds from distinct chemical classes were directly compared for efficacy and potency in hone, uteri, lipids, adipose tissues an ovariectomized model with 6 month old rats. Five weeks of oral dosing confirmed that ethynyl estradiol, tamoxifen, raloxifene are potent inhibitors loss volumetric bone mineral density (BMD, mg/cc) induced by ovariectomy, as measured computed tomography. In metaphysis distal femora rats, analysis showed a significant 12-20% decrease (P< 0.01) BMD. Linear regression was used to calculate half-maximal efficacious doses estradiol ED(50) =0.04mg /kg, which threefold more than turn raloxifene, nafoxidine. uterus, had minimal effects on endometrium smaller uterine eosinophil peroxidase activity nafoxidine, or estrogen, respectively. Estrogen most reducing cholesterol levels whereas tamoxifen nafoxidine effective blocking gain body weight. Distinct advantages management bone, uterine, serum cholesterol, after ovariectomy. The pattern pharmacological may be best understood terms their respective structure, specifically estrogens, benzothiophenes (raloxifene), dihydronapthylenes (nafoxidine), triphenylethylenes (tamoxifen). These data point separate estrogen deficiency, show benzothiophene has potentially important over uterus.