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雷洛昔芬可维持去卵巢大鼠的骨强度和骨量。

Raloxifene preserves bone strength and bone mass in ovariectomized rats.

作者信息

Turner C H, Sato M, Bryant H U

机构信息

Department of Ortopaedic Surgery, Indiana University Medical Center, Indianapolis 46202.

出版信息

Endocrinology. 1994 Nov;135(5):2001-5. doi: 10.1210/endo.135.5.7956922.

DOI:10.1210/endo.135.5.7956922
PMID:7956922
Abstract

We investigated the effects of raloxifene, a nonsteroidal benzothiophene, on bone strength in ovariectomized rats and compared them with estrogen treatment. Sixty ovariectomized Sprague-Dawley rats were divided into three groups for treatment with orally dosed raloxifene (3 mg/kg), ethynyl estradiol (EE, 0.1 mg/kg), or vehicle. A fourth group of 20 rats that underwent sham ovariectomies and received vehicle was used for comparison. Treatments began 3 days after ovariectomy and continued for 6 months. Raloxifene treatment resulted in greater bone strength in the lumbar vertebrae (P < 0.05) and femoral neck (P < 0.01) and greater bone mineral density at the proximal tibia (P < 0.001) and lumbar vertebrae (P < 0.001) when compared with vehicle-treated ovariectomized animals. The positive effects on bone biomechanical properties from raloxifene treatment were not different than those associated with EE treatment. Raloxifene did not cause a significant increase in uterine weight, whereas EE treatment resulted in uterine weight increased 4-fold over vehicle-treated ovariectomized controls. Therefore, in rats, raloxifene has beneficial effects on bone biomechanics that are equivalent to those of EE treatment without substantial effects on the uterus.

摘要

我们研究了非甾体类苯并噻吩雷洛昔芬对去卵巢大鼠骨强度的影响,并将其与雌激素治疗效果进行比较。将60只去卵巢的斯普拉格-道利大鼠分为三组,分别口服给予雷洛昔芬(3毫克/千克)、乙炔雌二醇(EE,0.1毫克/千克)或赋形剂。另外选取20只接受假去卵巢手术并给予赋形剂的大鼠作为第四组用于对照。去卵巢3天后开始给药,持续6个月。与接受赋形剂治疗的去卵巢动物相比,雷洛昔芬治疗使腰椎(P<0.05)和股骨颈(P<0.01)的骨强度更高,胫骨近端(P<0.001)和腰椎(P<0.001)的骨矿物质密度更高。雷洛昔芬治疗对骨生物力学特性的积极影响与EE治疗的效果没有差异。雷洛昔芬不会使子宫重量显著增加,而EE治疗导致子宫重量比接受赋形剂治疗的去卵巢对照增加了4倍。因此,在大鼠中,雷洛昔芬对骨生物力学具有有益作用,其效果与EE治疗相当,且对子宫无实质性影响。

相似文献

1
Raloxifene preserves bone strength and bone mass in ovariectomized rats.雷洛昔芬可维持去卵巢大鼠的骨强度和骨量。
Endocrinology. 1994 Nov;135(5):2001-5. doi: 10.1210/endo.135.5.7956922.
2
A new selective estrogen receptor modulator, CHF 4227.01, preserves bone mass and microarchitecture in ovariectomized rats.一种新型选择性雌激素受体调节剂CHF 4227.01可维持去卵巢大鼠的骨量和骨微结构。
J Bone Miner Res. 2005 Dec;20(12):2178-88. doi: 10.1359/JBMR.050801. Epub 2005 Aug 1.
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Longitudinal and cross-sectional analysis of raloxifene effects on tibiae from ovariectomized aged rats.雷洛昔芬对去卵巢老龄大鼠胫骨影响的纵向和横断面分析
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Advantages of raloxifene over alendronate or estrogen on nonreproductive and reproductive tissues in the long-term dosing of ovariectomized rats.在长期给去卵巢大鼠给药时,雷洛昔芬相对于阿仑膦酸盐或雌激素在非生殖组织和生殖组织方面的优势。
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Dual-energy x-ray absorptiometry of raloxifene effects on the lumbar vertebrae and femora of ovariectomized rats.雷洛昔芬对去卵巢大鼠腰椎和股骨影响的双能X线吸收法测定
J Bone Miner Res. 1994 May;9(5):715-24. doi: 10.1002/jbmr.5650090517.
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Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats.雷洛昔芬(盐酸LY139481)可预防去卵巢大鼠的骨质流失并降低血清胆固醇,且不会引起子宫肥大。
J Clin Invest. 1994 Jan;93(1):63-9. doi: 10.1172/JCI116985.
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New bone formation with teriparatide [human parathyroid hormone-(1-34)] is not retarded by long-term pretreatment with alendronate, estrogen, or raloxifene in ovariectomized rats.在去卵巢大鼠中,阿仑膦酸盐、雌激素或雷洛昔芬的长期预处理不会抑制特立帕肽[人甲状旁腺激素-(1-34)]诱导的新骨形成。
Endocrinology. 2003 May;144(5):2008-15. doi: 10.1210/en.2002-221061.
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Raloxifene and vitamin K2 combine to improve the femoral neck strength of ovariectomized rats.雷洛昔芬与维生素K2联合使用可提高去卵巢大鼠的股骨颈强度。
Calcif Tissue Int. 2005 Aug;77(2):119-26. doi: 10.1007/s00223-004-0277-8. Epub 2005 Jul 28.
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LY353381.HCl: a novel raloxifene analog with improved SERM potency and efficacy in vivo.盐酸LY353381:一种新型雷洛昔芬类似物,在体内具有增强的选择性雌激素受体调节剂效力和功效。
J Pharmacol Exp Ther. 1998 Oct;287(1):1-7.
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LY353381 x HCl: an improved benzothiophene analog with bone efficacy complementary to parathyroid hormone-(1-34).LY353381盐酸盐:一种改良的苯并噻吩类似物,其骨骼功效与甲状旁腺激素-(1-34)互补。
Endocrinology. 1998 Nov;139(11):4642-51. doi: 10.1210/endo.139.11.6307.

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