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Hashimoto, Kazuyuki; Wan, K. W. H. B. B.*; Matsuoka, Hiromitsu
Journal of Nuclear and Radiochemical Sciences, 6(3), p.193 - 196, 2005/12
The radioisotopes of rhenium (Re and Re) are attractive radionuclides for radiotherapy because of their energetic beta particles and gamma rays suitable for imaging. Mercaptoacetyltriglycine, MAG3 (NS ligand), is a useful bifunctional ligand in labeling monoclonal antibodies with metallic radionuclides. In this study, the labeling of MAG3 with carrier-free Re from a W/Re generator was investigated in detail. The Re-MAG3 complex was synthesized by the direct labeling method and by the indirect labeling method using a transfer ligand (citric acid or gluconic acid). The dependence of the labeling yield upon the reaction conditions such as the concentrations of tin(II) chloride dihydrate as a reducing agent, S-benzoyl MAG3 and the transfer ligand, pH, temperature, reaction time and the addition of a carrier was examined. The labeling yield of Re-MAG3 synthesized by the all method was over 90% under the optimum conditions.
Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Ono, Masahiro*; Hanaoka, Hirofumi*; Ishino, Seigo*; Hashimoto, Kazuyuki; Nishimura, Hiroshi*; Saji, Hideo*
Bioconjugate Chemistry, 16(4), p.751 - 757, 2005/07
Times Cited Count:61 Percentile:86.86(Biochemical Research Methods)Rhenium-186-1-hydroxyethylidene-1,1-diphosphonate (Re-HEDP) has been used for the palliation of metastatic bone pain. Delayed blood clearance and high gastric uptake of radioactivity have been observed upon injection, due to the instability of Re-HEDP in vivo. In this study, on the basis of the concept of bifunctional radiopharmaceuticals, we designed a stable Re-mercaptoacetylglycylglycylglycine (MAG3) complex-conjugated bisphosphonate (Re-MAG3-HBP). After purification by HPLC, Re-MAG3-HBP was synthesized with a radiochemical purity of over 95%. In biodistribution experiments, the radioactivity level ofRe-MAG3-HBP in bone was significantly higher than that of Re-HEDP. Blood clearance of Re-MAG3-HBP was faster than that of Re-HEDP. In addition, the gastric accumulation of Re-MAG3-HBP radioactivity was lower than that of Re-HEDP. In conclusion, Re-MAG3-HBP is expected to be a useful radiopharmaceutical for the palliation of metastatic bone pain.
Japan-Russia Seminar on Utilization of Radiation and Radioisotopes for Medical Purposes, 0, p.1 - 12, 1994/00
no abstracts in English
Hashimoto, Kazuyuki; Kawabata, Masako*; Saeki, Hideya*; Sato, Shunichi*; Tsukada, Kazuaki; Watanabe, Satoshi; Nagai, Yasuki
no journal, ,
no abstracts in English
Hashimoto, Kazuyuki; Kawabata, Masako*; Saeki, Hideya*; Sato, Shunichi*; Tsukada, Kazuaki; Hatsukawa, Yuichi; Nagai, Yasuki; Watanabe, Satoshi; Ishioka, Noriko
no journal, ,
no abstracts in English