• Journal of Radiopharmaceuticals and Molecular Probes
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• v.2 no.2
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• pp.123-131
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• 2016

Increasing clinical demand for carbon-11 labeled radiopharmaceuticals has triggered technological advances in fields of radiochemistry and automated modules. Even though carbon-11 has a short half-life ($t_{1/2}=20.4min$), the consecutive second production of carbon-11 labeled radiopharmaceutical in one $^{11}C$-synthetic module should be delayed at least over 4 h to avoid the high radiation exposure. We herein aimed to produce two different carbon-11 labeled radiopharmaceuticals ([$^{11}C$]PIB and [$^{11}C$]methionine) by sharing of [$^{11}C$]methylation source in one $^{11}C$-synthetic module. The synthesis of $^{11}C$-labeling reagents ($[^{11}C]CH_3I$ or $[^{11}C]CH_3OTf$) is fully automated using the commercial TRACERlab $FX_{C-pro}$ module and is readily adaptable to $^{11}C$-labeling reactor for [$^{11}C$]PIB as well as another $^{11}C$-labeling apparatus for [$^{11}C$]methionine via the three-way valve. After completing the [$^{11}C$]PIB production, the re-synthesized $[^{11}C]CH_3I$ was passed through the three-way valve connected the polyetheretherketone (PEEK) line and loaded into the C18 Sep-Pak cartridge including the methionine precursor. The labeled product [^${11}C$]methionine was purified by a simple cartridge separation and reformulated into saline. The radiochemical yield of [$^{11}C$]PIB and [$^{11}C$]methionine were $5.3{\pm}0.6%$ and $18.7{\pm}0.8%$ (n.d.c.), respectively, with over 97% of radiochemical purity. The specific activity of [$^{11}C$]PIB was over $110GBq/{\mu}mol$. Total production time of two radiopharmaceuticals needs about 2 h from $1^{st}$ beam irradiation including quality control tests. Final [$^{11}C$]PIB and [$^{11}C$]methionine were satisfied all quality control test standards.

• Bulletin of the Korean Chemical Society
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• v.26 no.1
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• pp.91-96
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• 2005

O-(3-[$^{18}$F]Fluoropropyl)-L-tyrosine (L-[$^{18}$F]FPT) was synthesized by nucleophilic radiofluorination followed by acidic hydrolysis of protective groups and evaluated with 9 L tumor bearing rat. L-[$^{18}$F]FPT is an homologue of O-(2-[$^{18}$F]fluoroethyl)-L-tyrosine (L-[$^{18}$F]FET) which recently is studied as a tracer for tumor imaging using positron emission tomography (PET). [$^{18}$F]FPT was directly prepared from the precursor of O-(3-ptoluenesulfonyloxypropyl)- N-(tert-butoxycarbonyl)-L-tyrosine methyl ester. FPT-PET image was obtained at 60 min in 9 L tumor bearing rats. The radiochemical yield of [$^{18}$F]FPT was 0-45% (decay corrected) and the radiochemical purity was more than 95% after HPLC purification. The total time elapsed for the synthesis of [$^{18}$F]FPT was 100 min from EOB (End-of-bombardment). A comparison of uptake studies between [$^{18}$F]FPT and [$^{18}$F]FET was performed. In biodistribution, [$^{18}$F]FPT showed similar pattern with [$^{18}$F]FET in various tissues, but [$^{18}$F]FPT showed low uptake in brain. Furthermore, [$^{18}$F]FPT showed higher tumor-to-brain ratio than [$^{18}$F]FET. In conclusion, [$^{18}$F]FPT seems to be more useful amino acid tracer than [$^{18}$F]FET for brain tumors imaging with PET.

• Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
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• v.13 no.2
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• pp.123-130
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• 2015

For the analysis of ⁹⁰Sr, which is a pure beta emitter, radiochemical separation from the main interfering elements such as Ca, Ba and Ra is required due to their similarity in chemical behavior to strontium. This study describes a radioanalytical procedure using extraction chromatography for separating Sr from interfering elements. The maximum capacity of the resin for Sr was approximately 6 mg per 1.5 mL of bed volume (BV). The recovery of Sr on the resin 1.5 mL (BV) was quantitative for the calcium level of 200 mg at the flow rate of 1 mL min^-1. However the chemical yield declined by increasing the flow rate by up to 5 mL min^-1 even at the calcium level of 200 mg. When using the same BV of Sr resin, the performance of the resin was enhanced as the cross-sectional area of the Sr resin column is small.

• The Korean Journal of Nuclear Medicine
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• v.12 no.1
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• pp.37-40
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• 1978

Labelling auflatoxines, the potential carcinogenic compounds, by radioactive iodine has been studied. The auflatoxine-$B_1$, which is known to be the most abundant components of auflatoxines in the nature, was labelled by radioactive iodine-125 through an acid catalyst chloroamine-T procedure. The radiochemical yield was amounted to 63.6%. The chemical structure of the labelled product was proved to be 6-iodo 5-methoxy coumarine structure of auflatoxine-$B_1$ molecule by means of I.R. and N.M.R. spectroscopy. The labelled product was orally administered in a test animal (Rat) and examined the accumnulation of radioactivity in the body at the definite time interval. The accumnulation of the radioactivity was pronounced at the blood and the liver. There was no indication of the decomposition of auflatoxine-$B_1-^{125}I$ in the organs of the test animal.

• Nuclear Engineering and Technology
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• v.48 no.3
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• pp.613-623
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• 2016

Molybdenum-99 ($^{99}Mo$) is the most important isotope because its daughter isotope, technetium-99m ($^{99m}Tc$), has been the most widely used medical radioisotope for more than 50 years, accounting for > 80% of total nuclear diagnostics worldwide. In this review, radiochemical routes for the production of $^{99}Mo$, and the aspects for selecting a suitable process strategy are discussed from the historical viewpoint of $^{99}Mo$ technology developments. Most of the industrial-scale $^{99}Mo$ processes have been based on the fission of $^{235}U$. Recently, important issues have been raised for the conversion of fission $^{99}Mo$ targets from highly enriched uranium to low enriched uranium (LEU). The development of new LEU targets with higher density was requested to compensate for the loss of $^{99}Mo$ yield, caused by a significant reduction of $^{235}U$ enrichment, from the conversion. As the dramatic increment of intermediate level liquid waste is also expected from the conversion, an effective strategy to reduce the waste generation from the fission $^{99}Mo$ production is required. The mitigation of radioxenon emission from medical radioisotope production facilities is discussed in relation with the monitoring of nuclear explosions and comprehensive nuclear test ban. Lastly, the $^{99}Mo$ production process paired with the Korea Atomic Energy Research Institute's own LEU target is proposed as one of the most suitable processes for the LEU target.

• Biomedical Science Letters
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• v.3 no.2
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• pp.131-138
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• 1997

IgG-$^{188}$Re conjugate was prepared for the diagnosis of abscess. The IgG molecules reduced by 2-mercaptoethanol contained 1.5 free sulfhydryl groups per IgG molecule. The reduced IgG molecule was labelled with $^{188}$Re through chelate to 99％ of labelling yield. The radiochemical purity of IgG-$^{188}$Re conjugate was maintained at 90％ in the presence of human serum for 1 hour. The IgG-$^{188}$Re was intravenously administered into staphylococcal abscess-bearing rats and their biodistribution was monitored at 4 and 24 hours post injection. The IgG-$^{188}$Re conjugate was moderately localized in the abscess tissue. This result implies that the IgG-$^{188}$Re conjugate can be a tool for abscess diagnosis. This technique can be applied for the preparation of various monoclonal antibody labelled with $^{188}$Re.

• The Korean Journal of Nuclear Medicine
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• v.28 no.3
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• pp.331-337
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• 1994

In order to develop a $^{18}F$-labelled myocardial perfusion agent(flow tracer) for PET, $^{18}F$-labelled organic ammonium cations were synthesized and evaluated in relation to their biodistribution. Five quaternary organic ammonium compounds were labelled with $^{18}F$ in a side chain with moderate to good yields by direct introduction of $^{18}F$-fluoride. Radiochemical yields have been achieved in 30-40min by the precursors (tosylates) in dimethylsulfoxide 15-60% (decay corrected). The reaction was found to be autocatalyzed. A remote controlled procedure was developed in these synthesis. $^{18}F$-Labelling and HPLC-purification of com-pounds needed about 60 min(Yield; 7-20%). Up to now the two compounds N-4-[$^{18}F$]fluorobutyl-pyridinium cation(1) and N, N dibenzyl-4(2-[$^{18}F$]fluoroethyl)piperidinium cation(2) were investigated in relation to their biodistribution in mice. Compound 1 showed at 1 min post injection the high uptake of 19.22% ID/g organ in the myocardium but a following fast decline to 1.12% ID/g organ after 40min. Uptake of compound 2 was after 1min in the heart 5.90% ID/g organ but after 40min at the relative high value of 4.33% ID/g organ. Heart:blood ratio for compound(1) at 1 min was 8.3, at 40 min 2.6 for compound II 2.0(1min) and 15.0(40 min). As data of compound 2 showed greater heart uptake, slower myocardial release, and higher heart: blood ratios, compound 2 is a good candidate for further evaluation.

• The Korea Journal of Herbology
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• v.23 no.1
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• pp.117-125
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• 2008

Objectives : This study was to verify the Attributive Channel theory of herbal medicine. Methods : [$^{131}I$]iodohesperetin was synthesized, separated, and refined from hesperetin, the major component of Citrus species, followed by observing the biodistribution in an organism of C57 BL/6 mice with and without Lewis Lung Carcinoma. Results : Iodohesperetin 27.5 mg was obtained through column cliromatography after a reaction with 50 mg of Hesperitin and 8 mg of Nal. The radiochemical yield of [$^{131}I$]iodohesperetin synthesis was 25 % when checked with Radio TLC chromatography. [131I]iodohesperetin was most largely distributed in the stomach, lung and liver of C57BL/6 mouse. The highest %ID/g in stomach was 40 min, in lung and liver was 20 min after injection. The % ID/g of tumor tissue was comparable with that of blood. Conclusions : The fact that [$^{131}I$]iodocurcumin was most largely distributed in the stomach, lung and liver was related with the Attributive Channel theory. And there was no significant finding related to tumor cells.

• Bulletin of the Korean Chemical Society
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• v.34 no.11
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• pp.3243-3248
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• 2013

The tissue inhibitor of metalloproteinase-2 (TIMP-2) inhibits matrix metalloproteinases activity and modulates cellular proliferation and apoptosis. The human serum albumin-TIMP-2 with folic acid conjugate (termed HT2-folate) was synthesized to promote uptake through folate receptors (FRs), and a corresponding radio-labeled compound was prepared for tumor diagnosis by positron emission tomography (PET). $^{68}Ga$-NOTA-HT2-folate was synthesized from $^{68}Ga$ and the NOTA chelator with HT2-folate. The fusion protein was identified using MALDI-TOF mass spectrometry. The radioligand was prepared with a high radiochemical yield. Cell-surface association of $^{68}Ga$-NOTA-HT2-folate significantly increased over time in FR-positive tumor cells. In animal PET and biodistribution studies, tumor uptake was very high as early as 1 h after radioligand injection. Folate conjugation enhanced the selective receptor-targeting efficacy of HT2 in FRexpressing tumors, and its radioligand will be useful as an in vitro tool and for in vivo tumor diagnosis by PET imaging.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.8 no.2
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• pp.63-70
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• 2022

The development of myocardial perfusion imaging (MPI) agents has been motivated because coronary artery disease has been one of the leading causes of death worldwide since the 1960s. Several positron emission tomography (PET) MPI agents were developed, and ¹⁸F-labeled phosphonium cations were reported actively among them. In this study, we synthesized novel ¹⁸F-labeled phosphonium cations, (5-[¹⁸F]fluoropentyl)diphenyl(pyridin-2-yl)phosphonium and (2-(2-[¹⁸F]fluoroethoxy)ethyl)diphenyl(pyridin-2-yl)phosphonium, and evaluated potential as MPI agents. Two labeled compounds were synthesized via nucleophilic substitution reactions of ¹⁸F-fluoride with the appropriate tosylate precursor in the presence of Kryptofix 2.2.2 and K₂CO₃. MicroPET studies were performed in normal rats to evaluate in vivo distribution of radiolabeled phosphonium cations for 60 min. The radiolabeled compounds were synthesized with 5%-10% yield. The radiochemical purity of labeled compounds was > 98% by analytical HPLC, and the specific activity was > 11.8 GBq/µmol. The result of microPET studies of these labeled compounds in rats showed intense uptake in the myocardium at 30 and 60 min. The results suggest that these ¹⁸F-labeled novel phosphonium cations would have potential as promising candidates for myocardial perfusion imaging.