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Journal Articles

Production of highly purified no-carrier-added $$^{177}$$Lu for radioimmunotherapy

Watanabe, Satoshi; Hashimoto, Kazuyuki; Watanabe, Shigeki; Iida, Yasuhiko*; Hanaoka, Hirofumi*; Endo, Keigo*; Ishioka, Noriko

Journal of Radioanalytical and Nuclear Chemistry, 303(1), p.935 - 940, 2015/01

 Times Cited Count:6 Percentile:39.55(Chemistry, Analytical)

Journal Articles

The Possible interplanetary transfer of microbes; Assessing the viability of ${it Deinococcus}$ spp. under the ISS environmental conditions for performing exposure experiments of microbes in the Tanpopo mission

Kawaguchi, Yuko*; Yang, Y.*; Kawashiri, Narutoshi*; Shiraishi, Keisuke*; Takasu, Masako*; Narumi, Issey*; Sato, Katsuya; Hashimoto, Hirofumi*; Nakagawa, Kazumichi*; Tanigawa, Yoshiaki*; et al.

Origins of Life and Evolution of Biospheres, 43(4-5), p.411 - 428, 2013/10

 Times Cited Count:23 Percentile:24.44(Biology)

Journal Articles

Performance of a remotely located muon radiography system to identify the inner structure of a nuclear plant

Fujii, Hirofumi*; Hara, Kazuhiko*; Hashimoto, Shugo*; Ito, Fumiaki*; Kakuno, Hidekazu*; Kim, S.*; Kochiyama, Mami; Nagamine, Kanetada*; Suzuki, Atsuto*; Takada, Yoshihisa*; et al.

Progress of Theoretical and Experimental Physics (Internet), 2013(7), p.073C01_1 - 073C01_20, 2013/07

 Times Cited Count:19 Percentile:24.09(Physics, Multidisciplinary)

Journal Articles

Tolerance of anhydrobiotic eggs of the tardigrade ${it Ramazzottius varieornatus}$ to extreme environments

Horikawa, Daiki*; Yamaguchi, Ayami*; Sakashita, Tetsuya; Tanaka, Daisuke*; Hamada, Nobuyuki*; Yukuhiro, Fumiko*; Kuwahara, Hirokazu*; Kunieda, Takekazu*; Watanabe, Masahiko*; Nakahara, Yuichi*; et al.

Astrobiology, 12(4), p.283 - 289, 2012/04

 Times Cited Count:18 Percentile:29.62(Astronomy & Astrophysics)

We examined the hatchability of hydrated and anhydrobiotic eggs of the tardigrade ${it Ramazzottius varieornatus}$ to hatch after ionizing irradiation (helium ions), extremely low and high temperatures, and high vacuum. Anhydrobiotic eggs (50% lethal dose; 1690 Gy) were substantially more radioresistant than hydrated ones (50% lethal dose; 509 Gy). Anhydrobiotic eggs also have a broader temperature resistance compared with hydrated ones. Over 70% of the anhydrobiotic eggs treated at high and low temperatures, but all of the hydrated eggs failed to hatch. After exposure to high vacuum conditions, the hatchability of the anhydrobiotic eggs was comparable to that of untreated control eggs.

Journal Articles

Selective separation of samarium(III) by synergistic extraction with $$beta$$-diketone and methylphenylphenanthroline carboxamide

Hasegawa, Yuko*; Tamaki, Sayaka*; Yajima, Hirofumi*; Hashimoto, Bunji*; Yaita, Tsuyoshi

Talanta, 85(3), p.1543 - 1548, 2011/09

 Times Cited Count:29 Percentile:24.64(Chemistry, Analytical)

Journal Articles

Production of no-carrier-added $$^{177}$$Lu for radioimmunotherapy

Watanabe, Satoshi; Hashimoto, Kazuyuki; Hanaoka, Hirofumi*; Endo, Keigo*; Ishioka, Noriko

JAEA-Review 2010-065, JAEA Takasaki Annual Report 2009, P. 109, 2011/01

no abstracts in English

Journal Articles

Production of Lu-177 capable of labeling antibodies

Watanabe, Satoshi; Hashimoto, Kazuyuki; Watanabe, Shigeki; Iida, Yasuhiko*; Hanaoka, Hirofumi*; Endo, Keigo*; Ishioka, Noriko

JAEA-Review 2009-041, JAEA Takasaki Annual Report 2008, P. 109, 2009/12

no abstracts in English

Journal Articles

Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of $$^{186}$$Re-MAG3-conjugated bisphosphonate ($$^{186}$$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

 Times Cited Count:19 Percentile:42.81(Radiology, Nuclear Medicine & Medical Imaging)

We have developed a $$^{186}$$Re-MAG3 complex-conjugated bisphosphonate ($$^{186}$$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 $$^{186}$$Re-MAG3-HBP because it has been reported that the concurrent administration of $$^{rm 99m}$$Tc-MAG3 and drugs with high affinity for serum protein enhanced total clearance and tissue distribution. The protein binding of $$^{186}$$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 $$^{186}$$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.

Journal Articles

Design, synthesis, and evaluation of [$$^{188}$$Re]Organorhenium-labeled antibody fragments with renal enzyme-cleavable linkage for low renal radioactivity levels

Uehara, Tomoya*; Koike, Miho*; Nakata, Hideo*; Hanaoka, Hirofumi*; Iida, Yasuhiko*; Hashimoto, Kazuyuki; Akizawa, Hiromichi*; Endo, Keigo*; Arano, Yasushi*

Bioconjugate Chemistry, 18(1), p.190 - 198, 2007/01

 Times Cited Count:12 Percentile:53.48(Biochemical Research Methods)

Renal localization of radiolabeled antibody fragments constitutes a problem in targeted imaging and radiotherapy. To estimate the applicability of the molecular design to metallic radionuclides, [$$^{188}$$Re]tricarbonyl(cyclopentadienylcarbonate)rhenium ([$$^{188}$$Re]CpTR-COOH) was conjugated with maleoyl-glycyl-lysine to prepare [$$^{188}$$Re]CpTR-GK. The cleavage of the glycyl-lysine linkage of the compound generates a glycine conjugate of [$$^{188}$$Re]CpTR-Gly. [$$^{188}$$Re]CpTR-GK was conjugated to thiolated Fab fragments to prepare [$$^{188}$$Re]CpTR-GK-Fab. The biodistribution of radioactivity after injection of [$$^{188}$$Re]CpTR-GK-Fab was compared with that of [$$^{188}$$Re]CpTR-Fab. [$$^{188}$$Re]CpTR-GK-Fab exhibited significantly lower renal radioactivity levels than did [$$^{188}$$Re]CpTR-Fab. The analysis of urine samples collected for 6 h postinjection of [$$^{188}$$Re]CpTR-GK-Fab showed that [$$^{188}$$Re]CpTR-Gly was the major radiometabolite. In tumor-bearing mice, [$$^{188}$$Re]CpTR-GK-Fab significantly reduced renal radioactivity levels without impairing the radioactivity levels in tumor. These findings indicate that the molecular design of radioparmaceuticals labeled with metallic radionuclides can be useful by using a radiometal chelate of high inertness and by designing a radiometabolite of high urinary excretion when released from antibody fragments following cleavage of a glycyl-lysine linkage. This study also indicates that a change in chemical structure of a radiolabel attached to a glycyl-lysine linkage significantly affected enzymes involved in the hydrolysis reaction.

Journal Articles

Therapeutic effects of a $$^{186}$$Re-complex-conjugated bisphosphonate for the palliation of metastatic bone pain in an animal model

Ogawa, Kazuma*; Mukai, Takahiro*; Asano, Daigo*; Kawashima, Hidekazu*; Kinuya, Seigo*; Shiba, Kazuhiro*; Hashimoto, Kazuyuki; Mori, Hirofumi*; Saji, Hideo*

Journal of Nuclear Medicine, 48(1), p.122 - 127, 2007/01

We developed a highly stable rhenium-186 ($$^{186}$$Re)-MAG3 complex-conjugated bisphosphonate, ($$^{186}$$Re-MAG3-HBP), for the treatment of painful bone metastases. This agent showed a superior biodistribution as a bone-seeking agent in normal mice when compared with $$^{186}$$Re-HEDP. In this study, we evaluated the therapeutic effects of $$^{186}$$Re-MAG3-HBP using an animal model of bone metastasis. In the rats treated with $$^{186}$$Re-HEDP, tumor growth was comparable to that in untreated rats. In contrast, when $$^{186}$$Re-MAG3-HBP was administered, tumor growth was significantly inhibited. Allodynia induced by bone metastasis was attenuated by treatment with $$^{186}$$Re-MAG3-HBP or $$^{186}$$Re-HEDP, but $$^{186}$$Re-MAG3-HBP tended to be more effective. These results indicate that $$^{186}$$Re-MAG3-HBP could be useful as a therapeutic agent for the palliation of metastatic bone pain.

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:59 Percentile:11.88(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

Design of a radiopharmaceutical for the palliation of painful bone metastases; Rhenium-186-labeled bisphosphonate derivative

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Hanaoka, Hirofumi*; Hashimoto, Kazuyuki; Nishimura, Hiroshi*; Saji, Hideo*

Journal of Labelled Compounds and Radiopharmaceuticals, 47(11), p.753 - 761, 2004/11

 Times Cited Count:27 Percentile:36.55(Biochemical Research Methods)

no abstracts in English

Oral presentation

Therapeutic effects of a new $$^{186}$$Re-labeled bisphosphonate in a rat model of bone metastasis

Ogawa, Kazuma*; Mukai, Takahiro*; Asano, Daigo*; Kawashima, Hidekazu*; Hashimoto, Kazuyuki; Shiba, Kazuhiro*; Mori, Hirofumi*; Saji, Hideo*

no journal, , 

no abstracts in English

Oral presentation

Control of biodistribution of Rhenium-186-MAG3-conjugated bisphosphonate using a competitive inhibitor of protein binding

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

no journal, , 

Previously, based on the concept of bifunctional radiopharmaceuticals, we developed a highly stable$$^{186}$$Re-MAG3 complex conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP) for treatment of the painful bone metastases. We assumed that competitive inhibitors of protein binding might be useful for$$^{186}$$Re-MAG3-HBP because it has been reported that the concurrent administration between $$^{99m}$$Tc-MAG3 and drugs with high protein binding affinity produced competitive displacement at the specific binding sites and enhanced total clearance and tissue distribution. In this study, the displacement effect between $$^{186}$$Re-MAG3-HBP and several protein binding inhibitors were investigated. Effects of each competitive protein binding inhibitor were examined in in vitro human serum. Bucolome, ceftriaxione and cefazolin as displacers of human serum albumin (HSA) binding site I, and ibuprofen as a displacer of HSA binding site II were added to each serum before addition of $$^{186}$$Re-MAG3-HBP. As a result of in vitro study, the free fraction rate of $$^{186}$$Re-MAG3-HBP was significantly increased by the addition of ceftriaxone. In biodistribution studies, the loading ceftriaxone enhanced the clearance of radioactivity of $$^{186}$$Re-MAG3-HBP in blood and non-target tissues without the reduction of the bone accumulation. These findings suggested that the use of a protein binding competitive inhibitor would be effective for lowering the side effects of $$^{186}$$Re-MAG3-HBP.

Oral presentation

Preparation of $$^{188}$$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, , 

$$^{188}$$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 $$^{188}$$Re. The labeling method using bifunctional chelating agents require the conjugation of $$^{188}$$Re-complex to protein after radiolabeling with the bifunctional chelating agent. Then, we planned the preparation of a stable $$^{188}$$Re-labeled protein by a simple method. A7 monoclonal antibody was labeled by reacting $$^{188}$$Re(I) tricarbonyl precursor with A7 directly. $$^{188}$$Re labeled A7 was prepared with radiochemical yield of 23%. After purification, $$^{188}$$Re labeled A7 showed radiochemical purity over 98%. After 24 hours of incubation, about 93% of $$^{188}$$Re-A7 remained intact, which indicates $$^{188}$$Re-A7 is stable in vitro. In biodistribution experiment, 11.2% of the injected dose/g of $$^{188}$$Re-A7 accumulated in the tumor at 24 hours postinjection, and tumor to blood ratio was over 1.0 at the same time.

Oral presentation

Production of Lu-177 capable of labeling antibodies

Watanabe, Satoshi; Hashimoto, Kazuyuki; Watanabe, Shigeki; Iida, Yasuhiko*; Hanaoka, Hirofumi*; Endo, Keigo*; Ishioka, Noriko

no journal, , 

no abstracts in English

Oral presentation

TANPOPO: astrobiology exposure and micrometeoroid capture experiments; For understanding survival possibility of trans-space migration of microorganisms

Yokobori, Shinichi*; Yang, Y.*; Fujisaki, Kenta*; Kawaguchi, Yuko*; Kobayashi, Kensei*; Hashimoto, Hirofumi*; Kawai, Hideyuki*; Mita, Hajime*; Narumi, Issei; Okudaira, Kyoko*; et al.

no journal, , 

no abstracts in English

Oral presentation

Space exposure experiments of microorganisms as a part of TANPOPO; Astrobiology exposure and micrometeoroid capture experiments

Yokobori, Shinichi*; Yang, Y.*; Fujisaki, Kenta*; Kawaguchi, Yuko*; Hashimoto, Hirofumi*; Yamashita, Masamichi*; Yano, Hajime*; Okudaira, Kyoko*; Yoshimura, Yoshitaka*; Narumi, Issei; et al.

no journal, , 

no abstracts in English

Oral presentation

TANPOPO (Astrobiology Exposure and Micrometeoroid Capture Experiments on ISS-JEM KIBO); Investigation of possible survivability of microorganisms in space

Yokobori, Shinichi*; Fujisaki, Kenta*; Kawaguchi, Yuko*; Yang, Y.*; Fushimi, Hidehiko*; Hashimoto, Hirofumi*; Yamashita, Masamichi*; Yano, Hajime*; Okudaira, Kyoko*; Hayashi, Nobuhiro*; et al.

no journal, , 

no abstracts in English

Oral presentation

Production of Lu-177 capable of labeling antibodies

Watanabe, Satoshi; Hashimoto, Kazuyuki; Watanabe, Shigeki; Iida, Yasuhiko*; Hanaoka, Hirofumi*; Endo, Keigo*; Ishioka, Noriko

no journal, , 

no abstracts in English

50 (Records 1-20 displayed on this page)