Eisenhut M, Kristen P, Garnier-Moiroux A, zum Winkel K
Nuklearmedizin. 1984 Jun;23(3):119-22.
The biodistribution of a series of new 99mTc-benzylidenediphosphonate complexes (99mTc-BDP) in rats was found to vary considerably with substituents in the alpha (X) and para (R) position of the BDP ligands. From the in vivo behaviour of the 99mTc-BDP complexes the following conclusions could be drawn: 1. the blood clearance was accelerated by X = NH2; 2. the kidney uptake was decreased by X = OH; 3. the bone uptake was enhanced by X = OH and R = OH; and 4. R = Cl retarded the blood clearance, increased the kidney and lowered the bone uptake. A subcutaneously transplantable osteosarcoma was tested with 99mTc-BDP complexes as a bone lesion model. Although rapidly growing the osteosarcoma accumulated less activity than the femur diaphysis. The small amount of binding sites in the tumor tissue for osteotropic radiopharmaceuticals was attributed to the formation of necroses.
研究发现，一系列新型99mTc-亚苄基二膦酸盐配合物（99mTc-BDP）在大鼠体内的生物分布会因BDP配体α位（X）和对位（R）的取代基不同而有很大差异。从99mTc-BDP配合物的体内行为可以得出以下结论：1. 当X = NH2时，血液清除加快；2. 当X = OH时，肾脏摄取减少；3. 当X = OH且R = OH时，骨摄取增加；4. 当R = Cl时，血液清除减慢，肾脏摄取增加，骨摄取降低。用99mTc-BDP配合物作为骨病变模型对皮下可移植骨肉瘤进行了测试。尽管骨肉瘤生长迅速，但其摄取的活性低于股骨干。肿瘤组织中亲骨性放射性药物的结合位点较少是由于坏死的形成。
