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Takahashi, Hiroki; Kojima, Toshiyuki; Narita, Takahiro; Sakaki, Hironao; Komukai, Satoshi*
Proceedings of 3rd International Particle Accelerator Conference (IPAC '12) (Internet), p.3972 - 3974, 2012/07
Control System for LIPAc realizes the remote control and monitoring and data acquisition by use of EPICS. For the validations of each subsystem performance and the activity of IFMIF Accelerator design, it is very important data obtained by commissioning of LIPAc and each subsystem. To certainly archive the important data for LIPAc and to efficiently search the LIPAc data, for design and validation, we started developing Data Acquisition System (DAC) based on Relational Database (RDB) has been developed. The first design for DAC of LIPAc is configured (1) using PostgreSQL for RDB and (2) several RDB for data archiving to ensure the data archive performance and to consider the increasing data amount. In addition, (3) only one RDB for data search is included in DAC and users can search the data via this RDB. In this way, several RDB for DAC can behave only one RDB against users. In this article, the development status of DAC for LIPAc is presented.
Re-MAG3-conjugated bisphosphonate (Re-MAG3-HBP), an agent for treatment of painful bone metastasesOgawa, 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：23 Percentile：57.81(Radiology, Nuclear Medicine & Medical Imaging)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.
Re-complex-conjugated bisphosphonate for the palliation of metastatic bone pain in an animal modelOgawa, 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 (Re)-MAG3 complex-conjugated bisphosphonate, (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 Re-HEDP. In this study, we evaluated the therapeutic effects of Re-MAG3-HBP using an animal model of bone metastasis. In the rats treated with Re-HEDP, tumor growth was comparable to that in untreated rats. In contrast, when Re-MAG3-HBP was administered, tumor growth was significantly inhibited. Allodynia induced by bone metastasis was attenuated by treatment with Re-MAG3-HBP or Re-HEDP, but Re-MAG3-HBP tended to be more effective. These results indicate that Re-MAG3-HBP could be useful as a therapeutic agent for the palliation of metastatic bone pain.
Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Otaka, Akira*; Ueda, Masashi*; Uehara, Tomoya*; Magata, Yasuhiro*; Hashimoto, Kazuyuki; Saji, Hideo*
Nuclear Medicine and Biology, 33(4), p.513 - 520, 2006/05
Times Cited Count：54 Percentile：80.16(Radiology, Nuclear Medicine & Medical Imaging)To develop a radiopharmaceutical for the palliation of painful bone metastases based on the concept of bifunctional radiopharmaceuticals, we synthesized a bisphosphonate derivative labeled with rhenium-186 (Re) that contains a hydroxyl group at the central carbon of its bisphosphonate structure and attached a stable Re-MAMA chelate to the amino group of a 4-amino-butylidene-bisphosphonate derivative, Re-MAMA-HBP, and investigated the effect of a hydroxyl group at the central carbon of its bisphosphonate structure on the affinity for hydroxyapatite and biodistribution by conducting a comparative study with Re-MAMA-BP. Re-MAMA-HBP was prepared by a reaction with ReO
and SnCl
in citrate buffer after the deprotection of trityl groups of Tr-MAMA-HBP. After reversed phase HPLC, Re-MAMA-HBP had a radiochemical purity of over 95 %. Compared with Re-MAMA-BP, Re-MAMA-HBP showed a greater affinity for hydroxyapatite beads in vitro and accumulated a significantly higher level in the femur in vivo. Thus, the introduction of a hydroxyl group into Re complex-conjugated bisphosphonates would be effective in enhancing accumulation in bone. These findings provide useful information on the design of bone-seeking therapeutic 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 (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.
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：28 Percentile：61.65(Biochemical Research Methods)no abstracts in English
Mukai, Takahiro*; Ogawa, Kazuma*; Arano, Yasushi*; Ono, Masahiro*; Fujioka, Yasushi*; Izumo, Mishiroku; Konishi, Junji*; Saji, Hideo*
Journal of Labelled Compounds and Radiopharmaceuticals, 44(Suppl.1), p.S617 - S618, 2001/05
no abstracts in English
Ogawa, Kazuma*; Ono, Masahiro*; Fujioka, Yasushi*; Saji, Hideo*; Mukai, Takahiro*; Konishi, Junji*; Uehara, Tomoya*; Arano, Yasushi*; Onoma, Katsuyuki
Kaku Igaku, 37(5), P. 577, 2000/09
no abstracts in English
Re-labeled bisphosphonate in a rat model of bone metastasisOgawa, Kazuma*; Mukai, Takahiro*; Asano, Daigo*; Kawashima, Hidekazu*; Hashimoto, Kazuyuki; Shiba, Kazuhiro*; Mori, Hirofumi*; Saji, Hideo*
no journal, ,
no abstracts in English
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 stableRe-MAG3 complex conjugated bisphosphonate (Re-MAG3-HBP) for treatment of the painful bone metastases. We assumed that competitive inhibitors of protein binding might be useful forRe-MAG3-HBP because it has been reported that the concurrent administration between 
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 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 Re-MAG3-HBP. As a result of in vitro study, the free fraction rate of Re-MAG3-HBP was significantly increased by the addition of ceftriaxone. In biodistribution studies, the loading ceftriaxone enhanced the clearance of radioactivity of 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 Re-MAG3-HBP.
Takahashi, Naoki; Nakamura, Yoshinobu; Obu, Tomoyuki; Samoto, Hirotaka; Namatame, Toshihiro; Hoshi, Takahiro; Kurabayashi, Kazuaki; Mukai, Yasunobu; Kimura, Yuichi; Kurita, Tsutomu
no journal, ,
no abstracts in English
