• The Korean Journal of Nuclear Medicine
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• v.27 no.2
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• pp.223-232
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• 1993

Technetium labeled isonitrile analogues are widely used as myocardial perfusion imaging agents. We synthesized and characterized a new isonitrile compound, ethyl 3-isocyanobutyrate(EIB). Proton and $^{13}C$ NMR spectroscopy and thin layer chromatography with a $C_{18}$ coat was performed. EIB was easily labeled with $^{99m}TcO_4^-$- with sodium dithionite. The labeling efficiency measured by RP-HPLC was over 95%. The labeled product was stable with dilution in normal saline and with prolonged incubation at room temperature. There was no formation of secondary products or free $^{99m}TcO_4^-$. In vivo kinetics study of $^{99m}Tc$ (I) labeled EIB in rabbits showed adequate myocardial uptake, good contrast against lung background, and relatively rapid liver clearance. The heart to lung ratio was over 2.5 and the heart to liver ratio was approximately from 0.4 to 5 at 60 minutes post injection. Hepatic clearance of $^{99m}Tc-MIBI$ was faster ($t_{1/2}$=6 minutes) than that of $^{99m}Tc-MIBI$. In vivo kinetics observed in dog was similar to that in rabbit but there was faster gallbladder filling, and thus lower liver background. SPECT imaging of the canine myocardium showed favorable imaging characteristics. However, biodistribution in mice demonstrated a myocardial % injected dose/organ of less than 0.1%. This was thought to be due to interspecies difference in plasma esterase activity. In human plasma, $^{99m}Tc$ ( I ) labeled EIB was stable for at least 2 hours, without production of secondary products by HPLC. We conclude that ethyl 3-isocyanobutyrate may be a potential new myocardial perfusion imaging agent and deserves further investigation as to its usefulness for clinical use.

• Tuberculosis and Respiratory Diseases
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• v.55 no.3
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• pp.280-286
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• 2003

Background : $^{99m}Technetium$ methylene diphosphonates($^{99m}Tc$ MDP) bone scintigraphy is current method of choice for the detection of bone metastases, but whole body $^{18}F$-fluoro-deoxy-D-glucose positron emission tomography($^{18}FDG$ PET) offers superior spatial resolution and improved sensitivity. So we compared whole body $^{18}FDG$ PET with $^{99m}Tc$ MDP bone scintigraphy in patients with skeletal metastases from lung cancer. Patients and Methods : Ninety-two patients with lung cancer taken $^{18}FDG$ PET together with a $^{99m}Tc$ MDP bone scintigraphy within 1 month between March 2000 and March 2003 were investigated retrospectively. Results : The sensitivity, specificity and accuracy of the $^{99m}Tc$ MDP bone scintigraphy versus $^{18}FDG$ PET for the detection of bone metastases in lung cancers were 59% vs 82%, 71% vs 94%, and 68% vs 91%, respectively. In the diagnosis of bone metastases from lung cancer, $^{18}FDG$ PET was statistically superior to $^{99m}Tc$ MDP bone scintigraphy in its specificity and accuracy(p<0.0001). Conclusions : Whole body $^{18}FDG$ PET may be useful in detecting bone metastases among patients with lung cancer.

• Korean Journal of Radiology
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• v.24 no.11
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• pp.1142-1150
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• 2023

Objective: To evaluate ^99mtechnetium-three polyethylene glycol spacers-arginine-glycine-aspartic acid (^99mTc-3PRGD₂) single-photon emission computed tomography (SPECT)/computed tomography (CT) imaging for diagnosing lymph node metastasis of primary malignant lung neoplasms. Materials and Methods: We prospectively enrolled 26 patients with primary malignant lung tumors who underwent ^99mTc-3PRGD₂ SPECT/CT and ¹⁸F-fluorodeoxyglucose (¹⁸F-FDG) positron emission tomography (PET)/CT imaging. Both imaging methods were analyzed in qualitative (visual dichotomous and 5-point grades for lymph nodes and lung tumors, respectively) and semiquantitative (maximum tissue-to-background radioactive count) manners for the lymph nodes and lung tumors. The performance of the differentiation of lymph nodes with and without metastasis was determined at the per-lymph node station and per-patient levels using histopathological results as the reference standard. Results: Total 42 stations had metastatic lymph nodes and 136 stations had benign lymph nodes. The differences between metastatic and benign lymph nodes in the visual qualitative and semiquantitative analyses of ^99mTc-3PRGD₂ SPECT/CT and ¹⁸F-FDG PET/CT were statistically significant (all P < 0.001). The area under the receiver operating characteristic curve (AUC) in the semi-quantitative analysis of ^99mTc-3PRGD₂ SPECT/CT was 0.908 (95% confidence interval [CI], 0.851-0.966), and the sensitivity, specificity, positive predictive value, and negative predictive value were 0.86 (36/42), 0.88 (120/136), 0.69 (36/52), and 0.95 (120/126), respectively. Among the 26 patients (including two patients each with two lung tumors), 15 had pathologically confirmed lymph node metastasis. The difference between primary lung lesions in patients with and without lymph node metastasis was statistically significant only in the semi-quantitative analysis of ^99mTc-3PRGD₂ SPECT/CT (P = 0.007), with an AUC of 0.807 (95% CI, 0.641-0.974). Conclusion: ^99mTc-3PRGD₂ SPECT/CT imaging may notably perform in the direct diagnosis of lymph node metastasis of primary malignant lung tumors and indirectly predict the presence of lymph node metastasis through uptake in the primary lesions.

• Bulletin of the Korean Chemical Society
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• v.27 no.2
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• pp.243-250
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• 2006

Three novel potential metal ion chelating units have been synthesized and characterized: 5-hexylcarbamoyl-3,4-dihydroxythiophene-2-carboxylic acid methyl ester (5), 3-benzyloxy-4-hydroxythiophene-2,5-dicarboxylic acid bis-hexylamide (6), and 3,4-dihydroxythiophene-2,5-dicarboxylic acid bis-hexylamide (7). The crystal structure of 6 was obtained and suggests the presence of three distinct intramolecular hydrogen bonds, namely $[N_{amide}-H{\cdot}{\cdot}{\cdot}O]$ $[O-H{\cdot}{\cdot}{\cdot}O_{amide}]$ and $[N_{amide}-H{\cdot}{\cdot}{\cdot}S]$. Boron chelation with 5, 6 and 7 through the use of $BF_3, \;B(OH)_3 \;or \;B(OMe)_3$ was probed by $^1H$, $^{11}B$, and $^{13}C$ NMR spectroscopy. Technetium (I) chelation with 5, 6 and 7 was also studied via HPLC elutions using $[^{99m}Tc(CO)_3(OH_2)_3]^+$.

• The Korean Journal of Nuclear Medicine
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• v.23 no.2
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• pp.219-223
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• 1989

Inflammation scan using radiolabelled leukocytes has high sensitivity and specificity. Several methods for labelling leukocytes have been evaluated using P-32 diisopropyl fluorophosphate (DFP-32), H-3 thymidine, Cr-51 chromate, Ga-67 citrate and Tc-99m-sulfur colloid. In-111-oxine has proved so far to be the most reliable agent for labelling leukocytes. In-111-oxine is, however, expensive, not easily available when needed, and its radiation dose to leukocytes is relatively high. Moreover, resolution of the resultant image is relatively poor. Tc-99m is still the agent of choice because of, as compared with the indium, its favorable physical characteristics, lower cost and availability. Now the technique for labelling the leukocytes with technetium is successfully obtained using the lipophilic HAPAO with higher efficiency for granulocytes than for other cells. With this technique it is possible to label leukocytes in plasma to improve the viability of the leukocytes. Inflammation scan using Tc-99m-HMPAO has been evaluated in several laboratories, and difference in methods for separation and labelling accounts for difference in efficiency, viability and biodistribution of the labelled leukocytes. We performed inflammation scan using leukocytes labelled with Tc-99m-HMPAO in three dogs 24 hours after inoculation of live E. Coli and A. Aureus in their right abdominal wall. We separated mixed leukocytes by simple sedimentation using 6% hetastarch (HES) and labelled the leukocytes with Tc-99m-HMPAO in 20% cell free plama diluted with phosphate buffer solution(Fig. 1). Uptake was high in the liver and spleen but is was minimal in the lungs on whole body scan. Kidneys and intestine showed minimal activity although it was high in the urinary bladder(Fig. 2). Uptake of labelled leukocytes in the inflammation site was do(mite on 2 hour-postinjection scan and abscess was clearly delineated on 24 hour-delayed scan with high target-to-nontarget ratio(Fig. 3, 4). Inflammation scan using mixed leukocytes labelled with Tc-99m-HMPAO is very sensitive and specific in early detection of inflammation.

• Nuclear Engineering and Technology
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• v.54 no.4
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• pp.1449-1455
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• 2022

A radiotracer investigation was carried out in a Thermal Stratification Test Facility (TSTF) with objectives of investigating the dispersion and diffusion of radionuclide and effectiveness of the thermocline to minimize the radionuclide content in the hot water layer. Technetium-99m (^99mTc) as sodium pertechnetate was used as a radiotracer in the investigation. Qualitative analysis showed that a thermocline is formed within the TSTF and is effective in preventing the transport of radionuclide from bottom section to the top section of the facility. It was found that the radiotracer injected at the bottom of the pool took about 17.4 h to disperse from bottom to the top of the facility. The results of the investigation helped in understanding the effectiveness of hot water layer and thus to minimize the pool top radiation levels.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.6 no.2
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• pp.75-91
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• 2020

[^99mTc]Tc-Hexamethylpropylene amine oxime (HMPAO) is currently used as a regional cerebral blood flow imaging agent for single photon emission computed tomography (SPECT). The HMPAO ligand exists in two isomeric forms: d,l and meso showing different properties in vivo. Later studies indicated that brain uptake patterns of ^99mTc-complexes formed from separated enantiomers differed. Separation of enantiomers is difficult by fractional crystallizations method. Usually, the substance is obtained in low chemical yield in a time-consuming procedure. Furthermore, the final product still contains some impurity. So we have developed new efficient route for synthesis of R,R- and S,S-HMPAO enantiomeric compounds in 6-steps. Nucleophilic substitution (S_N2) reactions of 2,2-dimethylpropane-1,3-diamine either with S- (1a) or R-methyl2-chloropropanoate (1b) were performed to produce compounds R,R- (2a) or S,S-isomer (2b) derivatives protected with benzylchloroformate (Cbz), respectively. And then Weinreb amide and methylation reaction using Grignard reagent, oxime formation with ketone group and deprotectiion of Cbz group by hydrogenolysis gave S,S- (7a) or R,R-HMPAO (7b), respectively. Entaniomeric compounds were synthesied with high yield and purity without any undesired product. The 7a or 7b kits containing 10 ㎍ SnCl₂-2H₂O were labeled with ^99mTc with high radiolabeling yield (90%).

• The Korean Journal of Nuclear Medicine
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• v.14 no.2
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• pp.61-66
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• 1980

We studied four patients with muscle necrosis associated with acute renal failure to evaluate the diagnostic value of the bone scan in this disease. The illness followed carbon monoxide poisoning in two patients, acute physical exertion in one and contaminated intramuscular injection in the other. Whole-body rectilinear bone scans using technetium 99m-methyldiphosphonate were done. In all patients, increased muscle labelling at the regions of suspected muscle injury was showed, and in one, it was after normalization of serum muscle enzyme levels. In one patient, the bone scan was rechecked 8 months later and showed no residual abnormality. Above all, the site and precise extent of muscle injury could be detected and the degree of muscle labelling seemed to correlate with the severy of muscle injury. These findings suggest that isotope scanning may be useful in the diagnosis of patients with acute muscle necrosis.

• The Korean Journal of Nuclear Medicine
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• v.39 no.1
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• pp.26-33
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• 2005

Purpose: The purpose of this study is to evaluate migration of technetium-99m hexamethylpropylene amine oxime ($^{99m}Tc$-HMPAO) labeled immature and mature dendritic cells (DC) in the mouse. Methods: DC were collected from bone marrow (BM) of tibiae and femurs of mice. Immature and mature DC from BM cells were radiolabeled with $^{99m}Tc$-HMPAO. To evaluate the functional and phenotypic changes of DC from radiolabeling, the allogeneic mixed lymphocyte reaction (MLR) and fluorescence-activated cell sorting (FACS) analysis were performed before and after labeling with $^{99m}Tc$-HMPAO. Migration of intravenously injected DC (iv-DC) was assessed by serial gamma camera images of mice with or without subcutaneous tumor. Percent injected dose per gram (%ID/g) was calculated in lungs, liver, spleen, kidneys, and tumor through dissection of each mice after 24 hours of injection. Results: Labeling efficiency of immature and mature DC were $60.4{\pm}5.4%\;and\;61.8{\pm}6.7%$, respectively. Iv-DC initially appeared in the lungs, then redistributed mainly to liver and spleen. Migration of mature DC to spleen was significantly higher than that of immature DC ($38.3{\pm}4.0%\;vs.\;32.2{\pm}4.1%$ in control group, $40.4{\pm}4.1%\;vs.\;35.9{\pm}3.8%$ in tumor group; p<0.05). Migration to tumor was also significantly higher in mature DC than in immature DC ($2.4{\pm}0.3%\;vs\;1.7{\pm}0.2%$; p=0.034). Conclusion: Assessment of migration pattern of DC in mice was possible using $^{99m}Tc$-HMPAO labeled immature and mature DC. Migration of mature DC to spleen and tumor was higher than that of immature DC when they were i.v. injected.

• The Korean Journal of Nuclear Medicine
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• v.15 no.1
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• pp.45-49
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• 1981

The hot spot on liver scan was demonstrated by many authors in various conditions such as SVC obstruction, Budd-Chiari syndrome, liver abscess, hemangioma of liver, hepatic venoocclusive diseases, IVC obstruction, and tricuspid insufficiency. And the appearance of hot spot in SVC obstruction is due to unsual collateral circulation. But there was no report of this hots pot on liver scan in our country. We have recently observed one patient with SVC obstruction who shows well-defined area of increased radioactivity between right and left lobe of liver on liver scan using $^{99m}Tc-tin$ colloid, and demonstrated collateral circulations with RI venography using $^{99m}Tc-O_4$. The injection site of radiocolloid was left antecubital vein. This hot spot did not appear when the radiocolloid was injected into right leg vein. We report here this hot spot on liver scan in SVC obstruction with review of some liter atures.