Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for radionuclide therapy

Ogawa, Kazuma*; Mizuno, Yoshiaki*; Washiyama, Koshin*; Shiba, Kazuhiro*; Takahashi, Naruto*; Kozaka, Takashi*; Watanabe, Shigeki; Shinohara, Atsushi*; Odani, Akira*

Nuclear Medicine and Biology, 42(11), p.875 - 879, 2015/11

https://doi.org/10.1016/j.nucmedbio.2015.07.001

Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of Re-MAG3-conjugated bisphosphonate (Re-MAG3-HBP), an agent for treatment of painful bone metastases

Ogawa, Kazuma*; Mukai, Takahiro*; Kawai, Keiichi*; Takamura, Norito*; Hanaoka, Hirofumi*; Hashimoto, Kazuyuki; Shiba, Kazuhiro*; Mori, Hirofumi*; Saji, Hideo*

European Journal of Nuclear Medicine and Molecular Imaging, 36(1), p.115 - 121, 2009/01

https://doi.org/10.1007/s00259-008-0925-8

We have developed a Re-MAG3 complex-conjugated bisphosphonate (Re-MAG3-HBP) for the treatment of painful bone metastases. We assumed competitive inhibitors of protein binding to be useful for procuring a favorable biodistribution of Re-MAG3-HBP because it has been reported that the concurrent administration of Tc-MAG3 and drugs with high affinity for serum protein enhanced total clearance and tissue distribution. The protein binding of Re-MAG3-HBP in a human serum albumin solution was significantly decreased by the addition of ceftriaxone. In the biodistribution experiments, pretreatment with ceftriaxone enhanced the clearance of the radioactivity of Re-MAG3-HBP in blood and nontarget tissues but had no effect on accumulation in bone. The findings suggested that the use of protein-binding competitive inhibitors would be effective in improving the pharmacokinetics of radiopharmaceuticals with high affinity for serum protein.

Fuel Failure Simulation Test in JOYO; FFDL in-pile test(III)

Ito, Chikara; Ito, Hideaki; Ishida, Koichi; Hatoori, Kazuhiro; Oyama, Kazuhiro; Sukegawa, Kazuya*; Murakami, Takanori; Kaito, Yasuaki; Nishino, Kazunari; Aoyama, Takafumi; et al.

JNC TN9410 2005-003, 165 Pages, 2005/03

JNC-TN9410-2005-003.pdf:12.66MB

At experimental fast reactor JOYO, appraisal of detection efficiency of behavior and FFD and FFDL of the fission product which is discharged inside the furnace as one of safety research of the country, is carried out. In MK-II core, the slit in the gas plenum part of the test sub-assembly, the test which irradiates this(1985 April, FFDL in-pile test(I)), providing the slit in the fuel column part of the test sub-assembly, the test which it irradiates(1992 November, FFDL in-pile test(II)) were carried out.MK-III reactor core replacement was completed and started in 2004. That the behavior in the system of FP with the reactor core replacement and so on changes in the MK-III reactor core and to have an influence on the sensitivity and the replying of FFD and FFDL are thought of. Therefore, behavior of FP in the fuel failure in the MK-III reactor core, the performance of FFD and FFDL must be confirmed beforehand. Moreover, to prepare for the fuel failure and the RTCB test which is doing a future plan, and to confirm a plant operation procedure in the fuel failure in MK-III reactor core operation and to attempt for the correspondency to improve are important.Therefore, in the period from 2004 November 11th to November 29th, it carried out the FFDL in-pile(III). It did a series of plant operation to stop a nuclear reactor after loading a reactor core center with the fuel element for the test which provided an artificial slit for the fuel cladding in the MK-III reactor core and irradiating it and detecting fuel damaging and to take out fuel. And it confirmed the operation procedure of the fast reactor in the fuel failure.Also, the improvement items such as the improvement of the operation and the procedure and the remodeling and the service of the facilities could be picked up. In the future, it attempts these compatible, and it prepares for the MK-III reactor core operation and it incorporates a final examination result by the improvement of the safety of FBR.

Summary Report of the Experimental Fast Reactor JOYO MK-III Performance Test

Maeda, Yukimoto; Aoyama, Takafumi; Yoshida, Akihiro; Sekine, Takashi; Ariyoshi, Masahiko; Ito, Chikara; Masaaki, Nemoto; Murakami, Takanori; Isozaki, Kazunori; Hoshiba, Hideaki; et al.

JNC TN9410 2003-011, 197 Pages, 2004/03

JNC-TN9410-2003-011.pdf:10.26MB

MK-III performance tests began in June 2003 to fully characterize the upgraded core and heat transfer system. Then, the last pre-use inspection was finished in November 2003.This report summarize the result of each performance test.

Preparation of Re-labeled antibody (A7) by a simple method using rhenium(I) tricarbonyl complex

Ogawa, Kazuma*; Kawashima, Hidekazu*; Kinuya, Seigo*; Yoshimoto, Mitsuyoshi*; Shiba, Kazuhiro*; Kimura, Hiroyuki*; Hashimoto, Kazuyuki; Mori, Hirofumi*; Saji, Hideo*

no journal, , 

Re is one of the most useful radionuclides for internal radiotherapy. However, there is a problem when protein such as antibody is used as a carrier of Re. The labeling method using bifunctional chelating agents require the conjugation of Re-complex to protein after radiolabeling with the bifunctional chelating agent. Then, we planned the preparation of a stable Re-labeled protein by a simple method. A7 monoclonal antibody was labeled by reacting Re(I) tricarbonyl precursor with A7 directly. Re labeled A7 was prepared with radiochemical yield of 23%. After purification, Re labeled A7 showed radiochemical purity over 98%. After 24 hours of incubation, about 93% of Re-A7 remained intact, which indicates Re-A7 is stable in vitro. In biodistribution experiment, 11.2% of the injected dose/g of Re-A7 accumulated in the tumor at 24 hours postinjection, and tumor to blood ratio was over 1.0 at the same time.