• 방사선산업학회지
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• 제4권1호
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• pp.13-17
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• 2010

The radioisotope labelling study was carried out for the sediment transport investigation. The fate of suspended solid materials is deeply related to the harbour siltation and the shoreline deformation that take place as a result of the artificial development of coastal area. In the experiment, $^{99m}TcO_4{^-}$ was chemically reduced and labelled in such a way that the labelled particles have the similar settling characteristics with the natural sediment. The radioisotope labelling techniques can be widely used for the natural resource exploration where the hydraulic dynamics of underground water and surface water are of importance.

• Bulletin of the Korean Chemical Society
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• 제32권7호
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• pp.2410-2412
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• 2011

Using a single step chemical synthesis, we synthesized the potential tumor imaging agent $^{99m}Tc$-diglucose-diethylenetriamine (DGTA) from diethylenetriamine and natural D-glucose. 10 min Incubation of 10 mg of precursor with 50 ${\mu}g$ of $SnCl_2{\cdot}2H_2O$ at room temperature yielded over 95% of $^{99m}Tc$ labeling. The stability for 6 hours in saline or human plasma was over 90%. In vitro tumor cell uptake assays using the SNU-C5 and 9 L cell lines showed that, in 0-400 mg/dL glucose medium, cell uptake of $^{99m}Tc$-DGTA was 1.5-8 times higher than that of [$^{18}F$]FDG. Moreover, [$^{18}F$]FDG uptake was dependent on glucose concentration in the medium, whereas cellular uptake of $^{99m}Tc$-DGTA was not dependent on glucose concentration, suggesting that the two compounds have different uptake mechanisms by tumor cells.

• Toxicological Research
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• 제29권1호
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• pp.21-25
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• 2013

The selective targeting of an integrin ${\alpha}_v{\beta}_3$ receptor using radioligands may enable the assessment of angiogenesis and integrin ${\alpha}_v{\beta}_3$ receptor status in tumors. The aim of this research was to label a peptidomimetic integrin ${\alpha}_v{\beta}_3$ antagonist (PIA) with $^{99m}Tc(CO)_3$ and to test its receptor targeting properties in nude mice bearing receptor-positive tumors. PIA was reacted with tris-succinimidyl aminotriacetate (TSAT) (20 mM) as a PIA per TSAT. The product, PIA-aminodiacetic acid (ADA), was radiolabeled with $[^{99m}Tc(CO)_3(H_2O)_3]^{+1}$, and purified sequentially on a Sep-Pak C-18 cartridge followed by a Sep-Pak QMA anion exchange cartridge. Using gradient C-18 reverse-phase HPLC, the radiochemical purity of $^{99m}Tc(CO)_3$-ADA-PIA (retention time, 10.5 min) was confirmed to be > 95%. Biodistribution analysis was performed in nude mice (n = 5 per time point) bearing receptor-positive M21 human melanoma xenografts. The mice were administered $^{99m}Tc(CO)_3$-ADA-PIA intravenously. The animals were euthanized at 0.33, 1, and 2 hr after injection for the biodistribution study. A separate group of mice were also co-injected with 200 ${\mu}g$ of PIA and euthanized at 1 hr to quantify tumor uptake. $^{99m}Tc(CO)_3$-ADA-PIA was stable in phosphate buffer for 21 hr, but at 3 and 6 hr, 7.9 and 11.5% of the radioactivity was lost as histidine, respectively. In tumor bearing mice, $^{99m}Tc(CO)_3$-ADA-PIA accumulated rapidly in a receptor-positive tumor with a peak uptake at 20 min, and rapid clearance from blood occurring primarily through the hepatobiliary system. At 20 min, the tumor-to-blood ratio was 1.8. At 1 hr, the tumor uptake was 0.47% injected dose (ID)/g, but decreased to 0.12% ID/g when co-injected with an excess amount of PIA, indicating that accumulation was receptor mediated. These results demonstrate successful $^{99m}TC$ labeling of a peptidomimetic integrin antagonist that accumulated in a tumor via receptor-specific binding. However, tumor uptake was very low because of low blood concentrations that likely resulted from rapid uptake of the agent into the hepatobiliary system. This study suggests that for $^{99m}Tc(CO)_3$-ADA-PIA to be useful as a tumor detection agent, it will be necessary to improve receptor binding affinity and increase the hydrophilicity of the product to minimize rapid hepatobiliary uptake.

• Bulletin of the Korean Chemical Society
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• 제30권5호
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• pp.1107-1112
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• 2009

The aim of this study is to develop and synthesize $5-HT_{1A}$ receptor imaging agents with WAY-100635 moiety and $^{99m}Tc(CO)_3$ core. WAY-100635 is commonly known as $5-HT_{1A}$ antagonist and its labeled compound ([$^{11}C$] WAY-100635) has been used as effective radioligand for imaging brain $5-HT_{1A}$ receptors with PET(Positron Emission Tomography). However, there are several restrictions in using a radioisotope of C-11 and requires for more effective radioisotopes and ligands. In order to produce a structure most similar to WAY-100635, WAY-100635 derivatives containing a cysteine chelator were designed and confirmed by using in silico (Hyperchem). The novel compounds (7a, 7b, 7c) were prepared in five or 7 steps with yields of 16%, 36% and 42%, respectively and radiolabeled with $[^{99m}Tc(CO)_3(H_2O)_3]^{+}$. The labeling yield was 99% for all the newly synthesized compounds. [$^{99m}Tc(CO)_3$]- WAY-100635 derivatives show a neutral charge which were confirmed by paper electrophoresis.

• 대한핵의학회지
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• 제36권6호
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• pp.333-343
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• 2002

목적: BFCA 중 하나인 HYNIC을 제조하고, 염증부위에 선택적으로 국소화 되어 진단할 수 있는 PEG-liposome과 결합시켜 HYNIC-PEG-liposome을 제조하며, 제조된 HYNIC-PEG-liposome에 방사성 동위원소인 $^{99m}Tc$의 표지 방법을 확립하고자 하였다. 대상 및 방법: 6-Chloronicotinic acid를 출발물질로 하여 succinimidyl 6-BOC-hydrazinopyridine-3-carboxylic acid를 순차적으로 합성하였다. Triethylamine을 이용해 합성된 succinimidyl 6-BOC-hydrazinopyridine-3-carboxylic acid와 DSPE를 접합하였다. HYNIC-DSPE를 제조한 후에 EPC:PEG-DSPE: HYNIC-DSPE:cholesterol을 1.85:0.15 :0.07:1의 몰 비로 혼합하여 HYNIC-PEG-liposome을 제조하였다. 제조된 HYNIC-PEG-liposome에 $SnCl_2{\cdot}2H_2O$와 tricine을 이용하여 $^{99m}Tc$를 표지하였다. $^{99m}Tc$-HYNIC-PEG-liposome과 혈청을 섞어서 실온과 $37^{\circ}C$에서 24시간까지 안정성을 확인하였다. $^{99m}Tc$-HYNIC-PEG-liposome에 DTPA, cysteine, glutathione을 각각 과량의 몰 비로 섞고 $37^{\circ}C$에서 1시간 반응 후에 trans- chelation을 통해 안정성을 확인하였다. 결과: 6-Chloronicotinic acid를 출발물질로 하여 6-hydrazinopyridine-3-carboxylic acid, 6-BOC-hydrazinopyridine -3-carb-oxylic acid, succinimidyl-6-BOC-hydra-zino-pyri- dine-3-carboxylic acid를 합성하였으며 각각의 합성수율은 88.5%, 93.7%, 93.2%였고 최종수율은 77.3%였다. 제조된 HYNIC-PEG-liposome의 직경은 106 nm였고, PEG-liposome에 접합된 HYNIC의 농도는 1.08 nM이었다. HYNIC-PEG- liposome의 개수는 1 ml에 $5.2{\times}10^{14}$개가 존재하였고, PEG- liposome 한 개당 HYNIC은 약 1250개가 접합되었다. 제조된 HYNIC-PEG-liposome에 $SnCl_2{\cdot}2H_2O$와 tricine을 이용하여 $^{99m}Tc$를 표지하였으며 그 표지수율은 99%이상이었다. 혈청 내에서 24시간까지 93.5% 이상의 안정성을 나타내었다. DTPA, cysteine, glutathione을 각각 1000배의 몰 비를 첨가한 경우 $^{99m}Tc$-HYNIC- PEG-liposome의 방사화학적순도가 각각 98%, 96%, 99%으로서 안정하였다. 결론: BFCA중 하나인 HYNIC을 이용한 $^{99m}Tc$-HYNIC-PEG-liposome의 제조는 손쉬운 표지방법과 높은 표지수율 그리고 안정성을 나타낼 수 있는 방법으로서, 이를 염증부위에 선택적으로 국소화되어 염증의 진단에 유용하게 사용될 수 있을것으로 기대된다.

• 대한방사성의약품학회지
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• 제5권1호
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• pp.18-25
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• 2019

2-Nitroimidazole derivatives have been reported to accumulate in hypoxic tissue. We prepared a novel $^{99m}Tc-MAG_3$-2-nitroimidazole and evaluated the feasibility for hypoxia imaging agent. $Bz-MAG_3$-2-nitroimidazole was synthesized by direct coupling of $Bz-MAG_3$ and 2-nitroimidazole using dicyclohexylcarbodiimide. $Bz-MAG_3$-2-nitroimidazole was labeled with $^{99m}Tc$ in the presence of tartaric acid and $SnCl_2-2H_2O$ at $100^{\circ}C$ for 30 min. And the reaction mixture was purified by $C_{18}$ Sep-pak cartridge. The labeling efficiency and the radiochemical purity were checked by ITLC-SG/acetonitrile. The tumor was grown in balb/c mice for 8~13 days after the subcutaneous injection of tumor cells, CT-26 (murine colon adenocarcinoma cell). Biodistribution study and tumor autoradiography were performed in the xenografted mice after i.v injection of 74 kBq/0.1 mL and 19 MBq/0.1 mL of $^{99m}Tc-MAG_3$-2-nitroimidazole, respectively. In vivo images of $^{99m}Tc-MAG_3$-2-nitroimidazole in tumor bearing mice were obtained 1.5 hr post injection. The labeling efficiency was $45{\pm}20%$ and the radiochemical purity after purification was over 95%. Paper electrophoresis confirmed negative charge of $^{99m}Tc-MAG_3$-2-nitroimidazole. $^{99m}Tc-MAG_3$-2-nitroimidazole was very stable at room temperature and its protein binding was 53%. The $^{99m}Tc-MAG_3$-2-nitroimidazole exhibited high uptake in the liver, stomach and intestine. In biodistribution study using tumor bearing mice, the uptakes (% ID/g) of the tumor were $0.5{\pm}0.1$, $0.4{\pm}0.0$, $0.2{\pm}0.1$ and $0.1{\pm}0.1$ at 5, 15, 30 min and 4 hrs. Tumor/muscle ratio were $1.4{\pm}0.1$, $2.2{\pm}0.83$, $3.0{\pm}0.9$, and 3.7 (n=2) for 5, 15, 30 min and 4 hrs. The uptake in hypoxic area was found higher than in non-hypoxic area of tumor tissue by autoradiography. In vivo images showed the relatively faint uptake to the hypoxic tumor region. $^{99m}Tc-MAG_3$-2-nitroimidazole was successfully synthesized and found feasible for imaging hypoxia.

• Journal of Radiation Protection and Research
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• 제40권4호
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• pp.231-243
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• 2015

Four different paddy soils collected around the Gyeongju nuclear site were treated with $^{99}TcO_4{^-}$ solution under the assumption of two contrasting contamination scenarios. Scenario I (SN-I) is for a pre-transplanting deposition of $^{99}Tc$ followed by plowing, whereas SN-II is for its deposition onto the water surface shortly after transplanting. Rice plants were grown in lysimeters in a greenhouse. Plant uptake of $^{99}Tc$ was quantified with the $TF_{area}$ ($m^2{\cdot}kg^{-1}-dry$). The SN-II $TF_{area}$ values for straws and brown rice, having been generally higher than the SN-I values, were within the ranges of $6.9{\times}10^{-3}{\sim}4.1{\times}10^{-2}$ and $5.2{\times}10^{-6}{\sim}7.3{\times}10^{-5}$, respectively. Sorption onto clay seems to have decreased $^{99}Tc$ uptake in SN-I, whereas it may have had an insignificant effect in SN-II. A phenomenon characteristic of submerged paddy soil, i.e., the development of a thin oxic surface layer may have greatly affected the rice uptake of SN-II $^{99}Tc$. The surface-water concentrations of $^{99}Tc$ were much higher in SN-II than in SN-I. For the percolating water, however, the opposite was generally true. At most 1.3% of the applied $^{99}Tc$ were leached through such percolation. The use of empirical deposition time-dependent $TF_{area}$ values was considered desirable in assessing the radiological impact of a growing-season deposition of $^{99}Tc$ onto paddy fields.

• 대한방사선기술학회지:방사선기술과학
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• 제46권5호
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• pp.401-408
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• 2023

Thyroid uptake measurements can be subject to measurement errors due to the scoping and positioning of the thyroid gland. To compensate for these limitations, the clinical utility of the thyroid simultaneous counting method as an alternative to thyroid uptake measurement was analyzed and evaluated experimentally through quantitative analysis of images acquired after thyroid scanning. Experimental data were obtained using a Gamma camera (GE infinia), a thyroid uptake system (KOROID 1), and a thyroid neck phantom. Based on the thyroid uptake rate of 1-5% according to the protocol of thyroid scan test (^99mTcO₄ - , 370 MBq) in normal results, ^99mTcO₄ - was set in the range of 3.7-18.5 MBq (Matrix: 256×256, Scan time: 1 min, collimator: pin hole, phantom-collimator distances: 7 cm). The acquired images were corrected for the attenuation of isotopes due to the set-up time and half-life by applying the Auto Region of interest (ROI) drawing system, and the significance of the experimental results was evaluated by Multiple linear regression analysis (SPSS, ver. 22, IBM). The thyroid uptake rate showed a significant correlation between the dose and the measured counts when using the thyroid uptake system equipment. Meanwhile, the quantitative analysis counts of phantom images using Gamma camera also showed a significant correlation. Thus confirmed that the correlation between these two experiments was statistically significant (P<0.05). The simultaneous counting protocol, which indirectly measures thyroid uptake from thyroid scans, is likely to be clinically relevant if complemented by additional studies with different variables in patients with thyroid disease.

• Bulletin of the Korean Chemical Society
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• 제32권7호
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• pp.2358-2368
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• 2011

Density functional theory (DFT) and time-dependent density functional theory (TDDFT) calculations, employing the B3LYP method and the LANL2DZ, 6-31G$^*$(LANL2DZ for Tc), 6-31G$^*$(cc-pVDZ-pp for Tc) and DGDZVP basis sets, have been performed to investigate the electronic structures and absorption spectra of the technetium-99m-labeled methylenediphosphonate ($^{99m}Tc$-MDP) complex of the simplest diphosphonate ligand. The bonding situations and natural bond orbital compositions were studied by the Mulliken population analysis (MPA) and natural bond orbital (NBO) analysis. The results indicate that the ${\sigma}$ and ${\pi}$ contributions to the Tc-O bonds are strongly polarized towards the oxygen atoms and the ionic contribution to the Tc-O bonding is larger than the covalent contribution. The electronic transitions investigated by TDDFT calculations and molecular orbital analyses show that the origin of all absorption bands is ascribed to the ligand-to-metal charge transfer (LMCT) character. The solvent effect on the electronic structures and absorption spectra has also been studied by performing DFT and TDDFT calculations at the B3LYP/6-31G$^*$(cc-pVDZ-pp for Tc) level with the integral equation formalism polarized continuum model (IEFPCM) in different media. It is found that the absorption spectra display blue shift in different extents with the increase of solvent polarity.

• 한국방사선학회논문지
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• 제9권4호
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• pp.235-238
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• 2015

소아 $^{99m}Tc-DMSA$ 검사에서 방광의 포함 여부에 따른 신장 섭취율의 차이를 비교 하였다. 팬텀실험과 임상실험으로 진행되었으며 3개의 컵으로 좌, 우측신장 그리고 방광에 위치시키고 좌, 우측 신장의 방사능은 일정한 양( 1.0 )으로 고정하였고 방광에 해당되는 컵에는 0, 0.5, 1, 2배 방사능의 차이를 두어 영상을 획득하였다. 임상환자는 $^{99m}Tc-DMSA$ (300uCi, 11MBq)을 주사하여 2시간 뒤 동일하게 영상 획득하여 각각 정량 분석하였다. 통계분석은 SPSS(ver 22.0) 으로 대응표본 T검증(paired T-test)을 사용하여 분석하였고 p<0.05는 통계적으로 유의하다고 판단하였다. 방광의 방사능을 제외한 양측 신장 섭취율은 $29.83{\pm}8.8%$(좌측), $24.29{\pm}6.66%$(우측)이었고, 방광을 포함했을 때 신장 섭취율은 $26.65{\pm}8.03%$(좌측), $21.78{\pm}6.24%$(우측)이었다. 신장 섭취율은 방광의 소변(방사능)이 증가할수록 양측 신장의 섭취율은 감소하였다. 이는 $^{99m}Tc-DMSA$ 신장스캔 시 좌, 우측 신장에서 방사능을 계수할 때 방광의 소변에 포함된 방사능의 계수가 포함되어 신장 섭취율 공식에서 총 계수가 포함되므로 실제 양측 신장 섭취율의 값이 감소되었다.