^(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

作　　者：付招娣[1] 陈晓光[1] 施波[1] 李燕[1] 雷小红[1] 夏丽娟[1] 韩锐[1] 

机构地区：[1]中国医学科学院

出　　处：《中国新药杂志》2004年第6期504-507,共4页Chinese Journal of New Drugs

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。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.

关 键 词：^153钐—乙二胺四亚甲基膦酸 止痛 骨侵袭 骨溶解 

分 类 号：R979.19[医药卫生—药品] R965.1[医药卫生—药学]