Search Results 1-20 of 101

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Initial Evaluation of AF78: a Rationally Designed Fluorine-18-Labelled PET Radiotracer Targeting Norepinephrine Transporter

Chen Xinyu , Fritz Alexander , Werner Rudolf A. , Nose Naoko , Yagi Yusuke , Kimura Hiroyuki , Rowe Steven P. , Koshino Kazuhiro , Decker Michael , Higuchi Takahiro

… Radiosynthesis of AF78 was undertaken, followed by validation in cell uptake studies, autoradiography, and in vivo imaging in rats.Results[18F]AF78 was successfully synthesized with 27.9 ± 3.1 % radiochemical yield, > 97 % radiochemical purity and > 53.8 GBq/mmol molar activity. …

Molecular Imaging and Biology 22(3), 602-611, 2019-07-22

IR
2

Trimodal Nanoparticle Contrast Agent for CT, MRI and SPECT Imaging: Synthesis and Characterization of Radiolabeled Core/Shell Iron Oxide@Gold Nanoparticles

Motiei Menachem , Dreifuss Tamar , Sadan Tamar , Omer Noam , Blumenfeld-Katzir Tamar , Fragogeorgi Eirini , Loudos George , Popovtzer Rachela , Ben-Eliezer Noam

… The particles showed efficient capabilities as CT/MRI imaging agent and high radiochemical yield, indicating a potential single hybrid material for multimodal SPECT/CT/MRI. …

Chemistry Letters 48(3), 291-294, 2019

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3

Study of 125I-EISB for Detecting Systematic Amyloidosis : Evaluation for optimal synthesis time and stability of 125I-EISB [in Japanese]

柏昂希 , 副島彩花 , 松永浩文 , 山下太郎 , 冨吉勝美

… We used high performance liquid chromatography (HPLC) to\acquire radiochemical purity of 125I-EISB. … We assess changes of radiochemical purity of 125I-EISB over time. … As a result, high radioactive purity 95.88±3.19% was obtained in 10 minutes by our synthesis and the radiochemical purity was 97.83±1.40% (n=6) applying our purification system. … Radiochemical purity 24 hours later was 94.01±2.09% after injecting in saline. …

熊本大学医学部保健学科紀要 (14), 42-47, 2018-03-31

IR Ichushi Web
4

Radioiodination of BODIPY and its application to a nuclear and optical dual functional labeling agent for proteins and peptides

Ono Masahiro , Watanabe Hiroyuki , Ikehata Yuki , Ding Ning , Yoshimura Masashi , Sano Kohei , Saji Hideo

… In the radioiodination reaction of BODIPY-NHS with [125I]NaI, [125I]BODIPY-NHS was obtained at a 48% radiochemical yield. … When we carried out the conjugation reaction of [125I]BODIPY-NHS with bovine serum albumin (BSA) and RGD (Arg-Gly-Asp) peptide as a model protein and peptide, respectively, [125I]BODIPY-BSA and [125I]BODIPY-RGD peptide were successfully prepared at 98 and 82% radiochemical yields, respectively. …

Scientific Reports (7), 2017-06-13

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5

Continuous-Flow Synthesis of N-Succinimidyl 4-[18F]fluorobenzoate Using a Single Microfluidic Chip

Kimura Hiroyuki , Tomatsu Kenji , Saiki Hidekazu , Arimitsu Kenji , Ono Masahiro , Kawashima Hidekazu , Iwata Ren , Nakanishi Hiroaki , Ozeki Eiichi , Kuge Yuji , Saji Hideo

… In the synthesis of [18F]SFB using this continuous-flow method, the three-step reaction was successfully completed within 6.5 min and the radiochemical yield was 64 ± 2% (n = 5). …

PLOS ONE 11(7), 2016-07-13

IR
6

Rapid isolation method for radioactive strontium using Empore™ Strontium Rad Disk

Zhang Zijian , Ninomiya Kazuhiko , Takahashi Naruto , Saito Takashi , Kita Kazuyuki , Yamaguchi Yoshiaki , Shinohara Atsushi

… The method employ ed solid-phase extraction and ion-exchange chromatography, and achieved a Sr yield of > …

Journal of Nuclear and Radiochemical Sciences 16(0), 15-21, 2016

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7

Gallium-68-labeled anti-HER2 single-chain Fv fragment: development and in vivo monitoring of HER2 expression.

Ueda Masashi , Hisada Hayato , Temma Takashi , Shimizu Yoichi , Kimura Hiroyuki , Ono Masahiro , Nakamoto Yuji , Togashi Kaori , Saji Hideo

… 【Results】[(68)Ga]Df-anti-HER2 scFv was obtained with high radiochemical yield after only a 5-min reaction at room temperature. …

Molecular imaging and biology 17(1), 102-110, 2015-02

IR
8

Development of the Fibronectin–Mimetic Peptide KSSPHSRN(SG)5RGDSP as a Novel Radioprobe for Molecular Imaging of the Cancer Biomarker α5β1 Integrin

Jin Zhao-Hui , Furukawa Takako , Kumata Katsushi , Xie Lin , Yui Joji , Wakizaka Hidekatsu , Fujibayashi Yasuhisa , Zhang Ming-Rong , Saga Tsuneo

… 18F-PR_b was produced with a labeling yield of 22.3±1.9% based on 18F-F−, a radiochemical purity of >99%, and a specific activity of 30–70 GBq/µmol; …

Biological and Pharmaceutical Bulletin 38(11), 1722-1731, 2015

J-STAGE Ichushi Web
9

Application of Microreactor to the Preparation of C-11-Labeled Compounds via O-[11C]Methylation with [11C]CH3I: Rapid Synthesis of [11C]Raclopride

Kawashima Hidekazu , Kimura Hiroyuki , Nakaya Yuta , Tomatsu Kenji , Arimitsu Kenji , Nakanishi Hiroaki , Ozeki Eiichi , Kuge Yuji , Saji Hideo

… Dimethyl sulfoxide solutions containing the O-desmethyl precursor or [11C]CH3I were introduced into separate injection ports by infusion syringes, and the radiochemical yields were measured under various conditions. … The decay-corrected radiochemical yield of microreactor-derived [11C]raclopride reached 12% in 20 s at 25 °C, which was observed to increase with increasing temperature. …

Chemical and Pharmaceutical Bulletin 63(9), 737-740, 2015

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10

The synthesis of [18F]pitavastatin as a tracer for hOATP using the Suzuki coupling.

Yagi Yusuke , Kimura Hiroyuki , Arimitsu Kenji , Ono Masahiro , Maeda Kazuya , Kusuhara Hiroyuki , Kajimoto Tetsuya , Sugiyama Yuichi , Saji Hideo

… Herein, we report a practical method for the synthesis of [(18)F]pitavastatin by the Suzuki coupling reaction of p-iodofluorobenzene and a quinoline boronate derivative, with the desired product being formed in a radiochemical yield of 12 ± 3% (decay corrected from [(18)F]fluoride ions, n = 3). …

Organic & biomolecular chemistry 13(4), 1113-1121, 2014-11-13

IR
11

Synthesis and evaluation of 18F-labeled mitiglinide derivatives as positron emission tomography tracers for β-cell imaging.

Kimura Hiroyuki , Matsuda Hirokazu , Fujimoto Hiroyuki , Arimitsu Kenji , Toyoda Kentaro , Mukai Eri , Nakamura Hiroshi , Ogawa Yu , Takagi Mikako , Ono Masahiro , Inagaki Nobuya , Saji Hideo

… (+)-(S)-o-[(18)F]FMIT was obtained with radiochemical yield of 18% by radiofluorination of racemic precursor 7, hydrolysis, and optical resolution with chiral HPLC; … its radiochemical purity was >99%. …

Bioorganic & medicinal chemistry 22(13), 3270-3278, 2014-07-01

IR
12

Study on the highly efficient synthesis of F^18-labeled radiopharmaceuticals [in Japanese]

Hayashi Kazutaka

Pharmaceutical bulletin of Fukuoka University 14(38), 87-97, 2014-03

IR
13

Preparation and characterization of cerium(IV) tellurium molybdate gel and its application as a bed for chromatographic 99Mo/99mTc generator

El-Amir M. A. , Mostafa M. , Ramadan H. E.

… The highest precipitation yield of 99Mo within the formed gel was found to be 97.6 % at a Ce:Te:Mo molar ratio of 1:0.2:1. … The 99mTc elution yield was 77.8±3.0 % with a radionuclidic purity of ≥ … 99.99 %, radiochemical purity of 96.5±1.3 % (as 99mTcO4-) and pH-value in the range of 5-7. …

Journal of Nuclear and Radiochemical Sciences 14(1), 1-5, 2014

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14

In Vivo Evaluation of a Radiogallium-Labeled Bifunctional Radiopharmaceutical, Ga-DOTA-MN2, for Hypoxic Tumor Imaging

Sano Kohei , Okada Mayumi , Hisada Hayato , Shimokawa Kenta , Saji Hideo , Maeda Minoru , Mukai Takahiro

… was achieved with high radiochemical yield (>85%) by 1-min of microwave irradiation (50 W). …

Biological and Pharmaceutical Bulletin 36(4), 602-608, 2013

J-STAGE Ichushi Web
15

Synthesis and evaluation of 2-chloro N-[(S)-{(S)-1-[11 C]methylpiperidin-2-yl} (phenyl)methyl]3- trifluoromethyl-benzamide ([11 C]N-methyl- SSR504734) as a PET radioligand for glycine transporter 1

Fuchigami Takeshi , Takano Akihiro , Gulyás Balázs , Jia Zhisheng , Finnema Sjoerd J , Andersson Jan D , Nakao Ryuji , Magata Yasuhiro , Haratake Mamoru , Nakayama Morio , Halldin Christer

… Results [11 C]N-methyl-SSR504734 was successfully synthesized in moderate radiochemical yield and high specific radioactivity. …

EJNMMI Research 2(1), 37, 2012-07-09

IR
16

Synthesis of [11C]uric acid, using [11C]phosgene, as a possible biomarker in PET imaging for diagnosis of gout

Yashio Keiji , Katayama Yumiko , Takashima Tadayuki , Ishiguro Naoki , Doi Hisashi , Suzuki Masaaki , Wada Yasuhiro , Tamai Ikumi , Watanabe Yasuyoshi

… The radiochemical yield of [11C]1 was 37 ± 7% (decay-corrected based on [11C]COCl2) with specific radioactivities of 96-152 GBq/μmol at the end of synthesis (n = 6). … The average time of radiosynthesis from the end of bombardment, including formulation, was about 30 min with >98% radiochemical purity. …

Bioorganic and Medicinal Chemistry Letters 22(1), 115-119, 2012-01-01

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17

5-O-(4-[125I]Iodobenzyl)-L-ascorbic Acid: Electrophilic Radioiodination and Biodistribution in Mice

Kim Jintaek , Kino Tomohiro , Kato Hiroharu , Yamamoto Fumihiko , Sano Kohei , Mukai Takahiro , Maeda Minoru

… agents for ascorbate bioactivity, 5-O-(4-[125I]iodobenzyl)-L-ascorbic acid ([125I]1) was prepared through a two-step sequence which involved radioiodo-destannylation of a protected tributylstannyl precursor 6, followed by hydrolysis in acidic methanol of the protecting groups in 61% overall radiochemical yield, with a radiochemical purity of over 98% and a specific activity of more than 15.4 GBq/μmol. …

Chemical and Pharmaceutical Bulletin 60(2), 235-240, 2012

J-STAGE Ichushi Web
18

Microwave-Assisted Synthesis of Organometallic Complexes of 99mTc(CO)3 and Re(CO)3: Its Application to Radiopharmaceuticals

Kimura Hiroyuki , Mori Daisuke , Harada Naoya , Ono Masahiro , Ohmomo Yoshiro , Kajimoto Tetsuya , Kawashima Hidekazu , Saji Hideo

… however, this method is poor in terms of chemical yield and reproducibility. … As a result, when water was used as the solvent under the irradiation of microwaves within 1 min, the Re(CO)3-PAMA complex could be directly synthesized from ethyl ester of PAMA (PAMAEE) and [Re(CO)3(H2O)3]Br in one step and with a high yield (94%). …

Chemical and Pharmaceutical Bulletin 60(1), 79-85, 2012

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19

A simple 18F-Acetate Synthesis and Purification and Quality Control for Clinical Use [in Japanese]

Miyazaki Yoshihiro , Ninomiya Kentaro , Takenaga Eriko , Yamano Masaki , Morishima Yoshitaka , Nomori Hiroyuki , Tomiyoshi Katsumi

… 18F-Actate radiochemical yield was 48.7% ± 5.2% (n-5). …

Bulletin of Kumamoto University, School of Health Sciences (8), 71-76, 2012

IR Ichushi Web
20

Efficient Synthesis of [11C]Ramelteon as a Positron Emission Tomography Probe for Imaging Melatonin Receptors Involved in Circadian Rhythms

Takashima-Hirano Misato , Tazawa Syusaku , Takahashi Kazuhiro , Doi Hisashi , Suzuki Masaaki

… First, [11C]methylation method showed the low reproducibility together with the production of many kinds of side products from which the [11C-methyl]Ramelteon was separated with chemical purity of <28% and radiochemical purity of >98%. …

Chemical and Pharmaceutical Bulletin 59(8), 1062-1064, 2011

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