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153钐-乙二胺四亚甲基膦酸的止痛和抗癌骨侵袭、骨溶解作用

The analgesic effect of ethylenediaminetetramethylene phosphonate ((153)~Sm-EDTMP) and its inhibitory effects on bone invasion and osteolysis of cancer in rats

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【作者】 付招娣陈晓光施波李燕雷小红夏丽娟韩锐

【Author】 FU Zhao-di,CHEN Xiao-guang,SHI Bo,LI Yan,LFI Xiao-hong,XIA Li-juan,HAN Rui( Institute of Materia Medica , Chinese Academy of Medical Sciences and PekingUnion Medical College, Beijing 100050, China )

【机构】 中国医学科学院中国医学科学院 中国协和医科大学药物研究所北京 100050中国协和医科大学药物研究所北京 100050

【摘要】 目的:研究153钐-乙二胺四亚甲基膦酸(153Sm-EDTMP)对动物疼痛的抑制和抗Walker 256癌的骨侵袭、骨溶解作用。方法:采用经典的物理和化学刺激致痛模型,观察给药后小鼠对热板刺激的痛阈、大鼠对光辐射刺激的甩尾阈以及化学物质刺激腹腔后的扭体反应,运用X光骨骼照片和胫骨病理切片,观察153Sm-EDTMP对Walker 256癌荷瘤大鼠的骨侵袭和骨溶解的影响。结果:153Sm-EUTMP静脉注射后2h已发挥止痛作用,尤以对光、热刺激后痛阈提高更明显,可持续2~4周。但其止痛强度和持续时间与注射剂量无明显相关。给药可抑制Walker 256癌的骨侵袭、骨溶解,74及148MBq·kg-1剂量组荷瘤大鼠遭受骨侵袭、骨溶解的胫骨数减少近一半。结 论:作为内照射用药,153Sm-EDTMP有明显的止痛和抗癌骨侵袭、骨溶解作用。

【Abstract】 Objective: To study the analgesic effect of 153Sm-EDTMP on animals and its inhibitory effect on bone invasion and osteolysis of Walker 256 carcinoma in rats. Methods:The analgesic effects were studied in mice by conventional methods such as heat plate,swing tail and twistings. The inhibition of bone invasion and osteolysis of Walker 256 carcinoma was evaluated in rats by X-ray and histological examination. Results: Data obtained indicated that 153Sm-EDTMP enhances the pain threshold of mice and rats but the analgesic duration had no clear dosage-effect relationship. Intra-venous injection of 74 or 148 MBq·kg-1 153Sm-EDTMP,the bone invasion and osteolysis in rats were reduced by 50% . Conclusion: 153Sm-EDTMP shows obvious analgesic effect and can inhibit bone invasion and osteolysis in rats caused by Walker 256 carcinoma.

  • 【文献出处】 中国新药杂志 ,Chinese New Drugs Journal , 编辑部邮箱 ,2004年06期
  • 【分类号】R96
  • 【被引频次】1
  • 【下载频次】59
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