生物活性 | |||
---|---|---|---|
描述 | Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. Diacerein (50mg/kg/day) was given orally to rats for 4 weeks in the presence or absence of cervical hyperkeratosis induced by intramuscular injection of Estradiol benzoate (60μg/100g) 3 times per week for 4 weeks. Estradiol benzoate succeeded to induce cervical hyperkeratosis which was detected by typical histopathological changes. In addition; there was significant reduction in superoxide dismutase levels and caspase-3 immunoexpression but significant increase in serum total cholesterol, malondialdehyde, total nitrites and interleukin-1b immunoexpression[2]. Administration of estradiol benzoate 1 week before cabergoline improved induction and synchronization of estrus in dogs[3]. In comparison with the controls, the mice treated with estradiol benzoate showed significantly decreased testicular indexes, no sperm in the sperm suspension or epididymal tubes, remarkably reduced numbers of spermatogonia, primary spermatocytes and Sertoli cells, down-regulated expression of PCNA and mRNA expressions of CyclinA1, CyclinB1, PCNA and VASA in the seminiferous tubules, but a dose-dependent increase of the p53 level[4]. Estradiol benzoate protective effect against MPP+ neurotoxicity is related to antioxidant effect of PON2 (paraoxonase-2), pro-inflammatory cytokines and GSHR but not to SOD2, catalase, GPX1 or GPX4[5]. |
临床研究 | |||||
---|---|---|---|---|---|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00650442 | Healthy | Phase 1 | Completed | - | United States, West Virginia ... 展开 >> Kendle International Inc. Morgantown, West Virginia, United States, 26505 收起 << |
NCT02670785 | Vulvovaginal Atrophy ... 展开 >> Menopause Dyspareunia 收起 << | Phase 2 | Completed | - | United States, Arizona ... 展开 >> Visions Clinical Research-Tucson Tucson, Arizona, United States, 85712 United States, California Genesis Center for Clinical Research San Diego, California, United States, 92103 United States, Connecticut Coastal Connecticut Research, LLC New London, Connecticut, United States, 06320 United States, Florida Women's Medical Research Group, LLC Clearwater, Florida, United States, 33759 Radiant Research, Inc. Pinellas Park, Florida, United States, 33781 Comprehensive Clinical Trials, LLC West Palm Beach, Florida, United States, 33409 United States, Georgia Fellows Research Alliance, Inc Savannah, Georgia, United States, 31406 United States, Michigan Beyer Research Kalamazoo, Michigan, United States, 49009 United States, Nevada Office of R. Garn Mabey, M.D. Las Vegas, Nevada, United States, 89128 United States, North Carolina Carolina Women's Research and Wellness Center Durham, North Carolina, United States, 27713 Hawthorne Medical Research, Inc. Winston-Salem, North Carolina, United States, 27103 United States, Ohio Rapid Medical Research, Inc. Cleveland, Ohio, United States, 44122 Women's Health Research Columbus, Ohio, United States, 43213 United States, Pennsylvania Clinical Research of Philadelphia, LLC Philadelphia, Pennsylvania, United States, 19114 United States, South Carolina Fellows Research Alliance, Inc Bluffton, South Carolina, United States, 29910 United States, Texas Radiant Research, Inc. Dallas, Texas, United States, 75231 Radiant Research, Inc. San Antonio, Texas, United States, 78229 United States, Virginia Virginia Women's Center Richmond, Virginia, United States, 23233 United States, Washington Seattle Women's Health, Research, Gynecology Seattle, Washington, United States, 98105 North Spokane Women's Clinic Spokane, Washington, United States, 99207 收起 << |
NCT03069781 | Muscle Atrophy | Early Phase 1 | Withdrawn(Lack of funding) | - | Canada, Ontario ... 展开 >> McMaster Univeristy Hamilton, Ontario, Canada 收起 << |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.66mL 0.53mL 0.27mL |
13.28mL 2.66mL 1.33mL |
26.56mL 5.31mL 2.66mL |
参考文献 |
---|