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Journal Articles

Labeling of bifunctional chelating agent, MAG3, with carrier-free $$^{188}$$Re

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 ($$^{186}$$Re and $$^{188}$$Re) are attractive radionuclides for radiotherapy because of their energetic beta particles and gamma rays suitable for imaging. Mercaptoacetyltriglycine, MAG3 (N$$_{3}$$S ligand), is a useful bifunctional ligand in labeling monoclonal antibodies with metallic radionuclides. In this study, the labeling of MAG3 with carrier-free $$^{188}$$Re from a $$^{188}$$W/$$^{188}$$Re generator was investigated in detail. The $$^{188}$$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 $$^{188}$$Re-MAG3 synthesized by the all method was over 90% under the optimum conditions.

Journal Articles

Development of a Rhenium-186-labeled MAG3-conjugated bisphosphonate for the palliation of metastatic bone pain based on the concept of bifunctional radiopharmaceuticals

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 ($$^{186}$$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 $$^{186}$$Re-HEDP in vivo. In this study, on the basis of the concept of bifunctional radiopharmaceuticals, we designed a stable $$^{186}$$Re-mercaptoacetylglycylglycylglycine (MAG3) complex-conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP). After purification by HPLC, $$^{186}$$Re-MAG3-HBP was synthesized with a radiochemical purity of over 95%. In biodistribution experiments, the radioactivity level of$$^{186}$$Re-MAG3-HBP in bone was significantly higher than that of $$^{186}$$Re-HEDP. Blood clearance of $$^{186}$$Re-MAG3-HBP was faster than that of $$^{186}$$Re-HEDP. In addition, the gastric accumulation of $$^{186}$$Re-MAG3-HBP radioactivity was lower than that of $$^{186}$$Re-HEDP. In conclusion, $$^{186}$$Re-MAG3-HBP is expected to be a useful radiopharmaceutical for the palliation of metastatic bone pain.

Journal Articles

Present status of radioisotope production for medical Applications by reactors in JAERI

Japan-Russia Seminar on Utilization of Radiation and Radioisotopes for Medical Purposes, 0, p.1 - 12, 1994/00

no abstracts in English

Oral presentation

Production of $$^{67}$$Cu for cancer therapy using accelerator neutrons

Hashimoto, Kazuyuki; Kawabata, Masako*; Saeki, Hideya*; Sato, Shunichi*; Tsukada, Kazuaki; Watanabe, Satoshi; Nagai, Yasuki

no journal, , 

no abstracts in English

Oral presentation

Production of $$^{67}$$Cu for cancer therapy with accelerator neutrons by deuterons

Hashimoto, Kazuyuki; Kawabata, Masako*; Saeki, Hideya*; Sato, Shunichi*; Tsukada, Kazuaki; Hatsukawa, Yuichi; Nagai, Yasuki; Watanabe, Satoshi; Ishioka, Noriko

no journal, , 

no abstracts in English

5 (Records 1-5 displayed on this page)
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