• The Korean Journal of Nuclear Medicine
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• v.24 no.1
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• pp.101-107
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• 1990

To develop $^{131}I-labelled$ m-iodobeneylguanidine $(^{131}I-MIBG)$, various experiments such as synthesis of MIBG, establishment of labelling conditions, determination of radiochemical purity, and examination of stability were carried out. 1) m-Iodobenzylguanidine (MIBG) sulfate was synthesized with a total yield of 62.4% by the condensation of m-iodobenzylamine hydrochloride with cyanamide via MIBG bicarbonate. Its physical properties, IR, $^1H-NMR$, and elemental analysis data were nearly identical to those of literature. 2) Freeze-dried or vacuum-dried kit vials were prepared from the mixture so as to contain MIBG (2 mg), ascorbic acid (10 mg), copper (II) sulfate (0.14 mg), and tin (II) sulfate (0.5 mg) per vial. Copper ( I ) catalyzed radioiodination of MIBG was carried out using kit vials and 0.01 M $H_2SO_4$ as solvent at $100^{\circ}C$ for 30 min under nitrogen atmosphere (optimal conditions). Labelling yield was 98% and radiochemical purity was 99.5%, respectively. 3) Solid-phase radioiodination of MIBG was carried out at $155^{\circ}C$ for 30 min using the prepared vials to contain MIBG (2 mg) and ammonium sulfate (10 mg). Duplicate reactions under the same conditions showed labelling yield of 95% and radiochemical purity of 99.5%. 4) $^{131}I-MIBG$ prepared either by catalytic or by solid-phase exchange method showed radio-chemical purity of 99% even after 3 days storing at room temperature.

• Journal of the Korean Chemical Society
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• v.11 no.2
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• pp.51-55
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• 1967

A procedure, which is effective enough to label various compounds at low temperature by radioactive iodine, was investigated. The chloramine-T procedure was mostly effective for labelling various protein, amino acids, hormones, and organic compounds by iodine, and the procedure was able to afford both high specific activity and high radiochemical yield. However, the procedure was ineffective for labelling unsaturated compounds or other organic compounds which has not active aromatic nucleus of reactive character. The radiochemical yield of the procedure was generally averaged from 100% to 60%. The reactivity of the aromatic part of the organic compound towards this reagent was correspond to that of an electrophillic reagent. The procedures were described and the reaction path was considered.

• Journal of Radiation Industry
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• v.4 no.1
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• pp.1-6
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• 2010

The purpose of this study is to synthesize the radio fluorine labelled isoquinoline salt derivative as new radiopharmaceutical for imaging tumors using positron emission tomography (PET). The planarity of isoquinoline allows to inhibit topoisomerase or intercalate between adjacent DNA base pairs, which result in producing double strand breaks in the DNA and a cell death. Therefore, the isoquinoline has seemed to have a potential anticancer activity. In order to obtain 2-(5-[$^{18}F$]fluoropentylisoquinolinium salt with good radiochemical yield, tosylated precursors have been synthesized. The labelling reaction was carried out for 30 minute in HMPA at $120^{\circ}C$. The radiochemical yield was about 50~60%.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.91-97
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• 2017

$^{18}F-THK-5351$ is a PET radiotracer to image the hyperphosphorylated tau fibrillar aggregates in human brain. This protocol describes the optimized radiosynthesis of $^{18}F-THK-5351$ using a commercial GE $TRACERlab^{TM}$ $FX_{FN}$ radiosynthesis module. $^{18}F-THK-5351$ was prepared by nucleophilic [$^{18}F$]fluorination from its protected tosylate precursors, (S)-(2-(2-methylaminopyrid-5-yl)-6-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy] quinolone(THK-5352), at $110^{\circ}C$ for 10 min in dimethyl sulfoxide, followed by deprotection with 1 N HCl. The average radiochemical yield of $^{18}F-THK-5351$ was $31.9{\pm}6.7%$(decay-corrected, n = 10), with molar activity of $198.1{\pm}33.9GBq/{\mu}mol$($5.4{\pm}0.9Ci/{\mu}mol$, n = 10). The radiochemical purity was determined to be above 98%. The overall production time including HPLC purification is approximately 70 min. This fully-automated protocol is validated for clinical use.

• The Korean Journal of Nuclear Medicine
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• v.23 no.1
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• pp.63-69
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• 1989

In order to develop technetium-99m-labelled human albumin microsphere (HAM) for lung scintigraphy, various experimemts such as preparation and fractionation of HAM, establishment of optimal labelling conditions, determination of radiochemical purity, stability test and biodistribution of $^{99m}Tc-HAM$ were carried out. HAM was prepared from the suspension of 1ml aqueous human serum albumin (25%) in 130 ml of olive oil at $130\sim135^{\circ}$ with vigorous stirring. The resulting HAM was fractionated with microsieve to get the desired particle size $(15\sim50\mu)$ and autoclaved for sterilizaiton. The HAM particles were treated with stannous chloride and the pH of the suspension was adjusted to $3.0\sim3.5$ with phosphate buffer. After freeze-drying the contents of single reaction vial containing 5 mg of HAM and 0.2 mg of $SnCl_2$ it was reacted with $Na^{99m}TcO_4$. The labelling yield was higher than 99.5% and the stability of $^{99m}Tc-HAM$ was high enough to maintain 99.1% of radiochemical purity up to 24 hours. Lung and liver uptake in mice was found to be 94% and 0.9%, respectively. Excellent rabbit and human lung scans were also obtained.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.5 no.2
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• pp.83-88
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• 2019

In order to understand the in vivo biodistribution of repebody protein (RB), an efficient and simple radiolabeling method for the protein is needed. We demonstrate a detailed protocol for the radiosynthesis of an ¹¹¹In radiolabeled tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctene-group conjugated repebody protein using inverse-electron-demand Diels-Alder reaction. First, 1,2,4,5-tetrazine (Tz) conjugated with a DOTA chelator, was used for preparing the radiolabeled DOTA complex with ¹¹¹In. Second, the trans-cyclooctene (TCO) functionalized repebody protein was synthesized which allows for the preparation of radiolabeled proteins by copper-free click chemistry. Following incubation with the ¹¹¹In-radiolabeled DOTA complex (¹¹¹In-Tz), the TCO-functionalized RB (TCO-RB) was radiolabeled successfully with ¹¹¹In, with a high radiochemical yield (69.5%) and radiochemical purity (>99%). The radiolabeling of repebody protein by copper-free click chemistry was accomplished within 20 min, with great efficiency in aqueous conditions. These results clearly indicate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.2 no.2
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• pp.103-107
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• 2016

Solid phase extraction (SPE) purification method is the efficient and well-known tool for automated [$^{11}C$]acetate synthesis. A fully automated homemade module adopting the SPE method and 'pinch' valves was developed very economically with a universal interface board, a relay card and an open source programmable logic controller. The radiochemical yield of the optimized [$^{11}C$]acetate synthesis by this system was $58.8{\pm}2.1%$ (n=10, decay-corrected) from $15.5{\pm}0.19GBq$ of $[^{11}C]CO_2$ as starting activity, and total synthetic time was 15 minutes. HPLC analysis showed its high radiochemical purity as $97.4{\pm}1.1%$ without possible by-products.

• Bulletin of the Korean Chemical Society
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• v.29 no.3
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• pp.595-598
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• 2008

Emodin (3-methyl-1,6,8-trihydroxyanthraquinone) is a natural chemotherapeutic compound with diverse biological properties including an antitumor activity. Emodin, a specific inhibitor of the protein tyrosine kinase, has a number of cellular targets in related to it. Its inhibition activity affects the mammalian cell cycle regulation in specific oncogene. Practically, it has been proven to inhibit HER-2/neu tyrosine kinase expressing breast cancer cells as an anticancer agent. 2-[123I]iodoemodin has been synthesized and evaluated human breast cancer cells (MDA-MB-231, MCF-7, fibroblast as a control) which express basal levels of HER-2/neu tyrosine kinase to investigate its suitability as a breast cancer imaging agent and 2-iodoemodin has been synthesized as a standard compound. The radiochemical yield of the 2-[123I]iodoemodin was about 72% and its radiochemical purity was over 97% after purification. The radioactivity of the 2-[123I]iodoemodin was increased in a time dependent manner in both cell lines and the ratio of MDA-MB-231 and MCF7 to fibroblast was 2.9 and 1.7, respectively.

• Bulletin of the Korean Chemical Society
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• v.19 no.9
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• pp.952-956
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• 1998

An automated system was developed for the routine preparation of carbon-11 ($^11C$) labeled radiopharmaceuticals, which consisted of three major parts including [$^11C$]methylation of the precursor with [$^11C$] iodomethane ($[^11C]CH_3I)$, purification of the desired product and formulation of the final $^11C$ labeled radiopharmaceutical. The whole system included seven three-way slider valves, eleven solenoid valves, four pneumatic cylinders, a HPLC (High Performance Liquid Chromatography) system and a rotary evaporator. Using this system, we investigated the radiochemical synthesis of L-[$methyl-^11C$]methionine, which is the most widely used amino acid in tumor PET (Positron Emission Tomography) studies. The overall operation took 3035 min including the production of $[^11C]CH_3I$ (10.5 min) and decay-corrected radiochemical yield was 25%. The automated system we described herein can be widely utilized for the preparation of many $^11C$ labeled radiopharinaceuticals and has been shown to be efficient, reliable and easy to operate.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.4 no.2
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• pp.90-94
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• 2018

The potential health risk from inhalational exposure of diesel exhaust particulates (DEP) has gained considerable scientific interests. However, the long-term in vivo behavior of DEP have not been clearly understood due to the difficulty of accurate analysis of these substances in a living subject. We herein demonstrate a detail protocol for the preparation of radiolabeled DEP using a radioactive-iodine-tagged pyrene analog. The purified $^{125}I$-labeled pyrene ($[^{125}I]1$) was obtained with a good radiochemical yield ($32{\pm}4%$, n=3) and high radiochemical purity (>99%) from the stannylated precursor 2. Next, the purified $[^{125}I]1$ was successfully assembled into the DEP suspension in an efficient manner. The radiolabeled DEP was highly stable in a mouse serum for 7 days without significant deiodination or dissociation of $[^{125}I]1$. These results clearly indicate that the present radiolabeling method will be useful for biodistribution study of carbonaceous particulates in vivo.