• The Korean Journal of Nuclear Medicine Technology
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• v.28 no.1
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• pp.1-11
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• 2024

Hypoxia, defined as the deficiency of oxygen, is a significant hallmark of cancers presenting in the majority of solid tumors. Detection of tumor hypoxia is essential in cancer diagnosis to prevent cancer progression, metastasis, and resistance to cancer therapies in clinical practices. Single-photon emission computed tomography (SPECT) is one of the methods studied and applied for hypoxia detection with the use of radiolabeled imaging agents in which ^99mTc is the common radioisotope used for radiolabeling. Nitroimidazoles are the hypoxia-targeting moieties presenting in numerous ^99mTc-radiolabeled imaging agents due to their bio-reducible ability in hypoxic environments. Recently, in addition to ^99mTc-labeled radiopharmaceuticals containing one nitroimidazole unit, there has been considerable attention given to ^99mTc-radiopharmaceuticals bearing two or more nitroimidazole units. This review summarizes the synthesis of hypoxia-targeting chelators and radiolabeling processes to produce these ^99mTc-radiopharmaceuticals for SPECT imaging.

• The Korean Journal of Nuclear Medicine Technology
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• v.20 no.2
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• pp.36-41
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• 2016

Purpose Sentinel lymphoscintigraphy (SLS) was using only $^{99m}Tc-phytate$. If the supply is interrupted temporarily, there is no alternative radiopharmaceuticals. The aim of this study measure the particle size of radiopharmaceuticals and look for radiopharmaceuticals which can be substituted for $^{99m}Tc-phytate$. Materials and Methods The particle size of radiopharmaceuticals were analyzed by a nano-particle analyzer. This study were selected known radiopharmaceuticals to be useful particle size for SLS. We were divided into control and experimental groups using $^{99m}Tc-DPD$, $^{99m}Tc-MAG3$, $^{99m}Tc-DMSA$ with $^{99m}Tc-phytate$. For in-vivo experiment, radiopharmaceuticals were injected intradermally at both foot to perform lymphoscintigraphy. Imaging was acquired to dynamic and delayed static image and observe the inguinal lymph nodes with the naked eye. Results Particle size was measured respectively Phytate 105~255 nm (81.9%), MAG3 91~255 nm (98.7%), DPD 105~342 nm (77.3%), DMSA 164~ 342 nm (99.2%), MAA 1281~2305 nm (90.6%), DTPA 342~1106 nm (79.4%), and HDP 295~955 nm (94%). In-vivo delayed static image, inguinal lymph nodes of all experiment groups and two control groups are visible to naked eye. however, $^{99m}Tc-MAG3$ of control groups is not visible to naked eye. Conclusion We were analyzed to the particle size of the radiopharmaceuticals that are used in in-vivo. Consequently, $^{99m}Tc-DPD$, $^{99m}Tc-DMSA $are possible in an alternative radiopharmaceuticals of emergency.

• Journal of Radiation Protection and Research
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• v.28 no.2
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• pp.117-125
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• 2003

It was reported that radiopharamaceuticals induced radiation adaptive response (RAR) in patients undergoing nuclear medicine imaging studies. Individual variations of RAR were not studied well. The purpose of this study was to evaluate individual variation of RAR in patients undergoing nuclear medicine imaging studies. Peripheral lymphocytes were collected from 23 patients undergoing $^{99m}Tc-diethylenetriamine$ pentaacetic acid $(^{99m}Tc-DTPA)$ renal scintigraphy, 18 patients undergoing $^{99m}Tc-methylene$ diphosphonate $(^{99m}Tc-MDP)$ bone scintigraphy and 21 patients undergoing $^{99m}Tc-tetrofosmin\;(^{99m}Tc-TF)$ scintigraphy were collected before and 4 hours after injection of radiopharmaceuticals. The lymphocytes were exposed to challenge dose of 2 Gy gamma rays using a cell irradiator. Numbers of ring-form (R) and dicentric (D) chromosomes were counted under the light microscope. and used to calculate the frequency of chromosomal aberration [Ydr=(D+R)/total number of counted lymphocytes]. Adaptation index (k) was defined 3s ratio of Ydr in conditioned lymphocytes over Ydr in unconditioned lymphocytes. Coefficients of variance of k in $^{99m}Tc-DTPA,\;^{99m}Tc-MDP\;and\;^{99m}Tc-TF$ were 35%, 34% and 21%, respectively k was not dependent upon age, sex, and underlying diseases. There was a wide variation of RAR induced by radiopharmaceuticals among patients undergoing nuclear medicine procedures. It remains to be determined for causes of such variation.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.1
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• pp.38-43
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• 2017

Tc-99m labeled sestamibi ($^{99m}Tc$-MIBI) is one of most widely used radiopharmaceuticals for myocardial SPECT imaging. Radiolabeling of $^{99m}Tc$-MIBI is recommended by heating in $100^{\circ}C$ water bath for 15 min. However, the water bath might be a source of contamination. Thus, if radiolabeling of $^{99m}Tc$-sestamibi can be performed at room temperature, then it would be more convenient to use in clinical application. In this study, we performed the radiolabeling of $^{99m}Tc$-MIBI in different temperature conditions or using different instruments to find out the efficient labeling condition. We studied the $^{99m}Tc$-MIBI labeling at room temperature or $100^{\circ}C$ heating block, and checked the labelling yields every 1 min for 10 min using radio-TLC with 2 different eluents-saline and acetone. From the experiment, we confirmed that the $^{99m}Tc$-MIBI can be labeled over 90% yield but not completed at room temperature. However, the $^{99m}Tc$-MIBI labeling was completed when it was performed in the $100^{\circ}C$ heating block. Finally, we proved that heating is essential for complete $^{99m}Tc$-MIBI labelling, furthermore using heating block is also possible instead of water bath.

• The Korean Journal of Nuclear Medicine
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• v.2 no.1
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• pp.67-71
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• 1968

Mercury bromo hydroxy propane-$Hg^{203},\;Tc-^{99m}$ colloidal, $Tc-^{99m}$ per technate (from $Tc-^{99m}$ Generator) were prepared and prepared products were tested their clinical usability to give agreeable results. Labelling of HSA by $Tc^{99m}$ and coagulation of HSA to MAA were conducted on a lab. scale. The iodine containning Radiopharmaceuticals; Hippuran, Sodiumiodide (inj), RISA, MAA, Rosebengal, Triolein, Phosphorus protein and $Mercury^{203}$ neohydrine were prepared by the conventional procedure. Total 206. 4 mC of Radiopharmaceuticals were prepared and 141.910 mC of them were distributed to the major users in this country.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.6 no.1
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• pp.3-9
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• 2020

Tetraiodothyroacetic acid (tetrac) is a derivative of thyroid hormone T₄ and causes anti-angiogenesis by blocking T₄ binding to integrin α_vβ₃. In this study, we synthesized [^99mTc]Tc-Cys-Asp-Gly(CDG)-tetrac and evaluated it in vitro as a tumor angiogenesis imaging ligand. The CDG was conjugated to tetrac as a chelator for technetium-99m labeling. The cold vial containing CDG-tetrac, sodium glucoheptonate, and reducing agent was completed under nitrogen-filled atmospheric glove bag. [^99mTc]Tc-CDG-tetrac was synthesized in quantitative yield by heating the cold vial with [^99mTc]TcO₄^- at 100℃ for 30 min. In vitro serum stability of [^99mTc]Tc-CDG-tetrac was measured by incubating the radioligand in 50% fetal bovine serum at 37℃ and analyzing the incubation mixture by radio-TLC, which showed high stability over 6 h (≥ 98%). Cell binding study was carried out by incubating [^99mTc]Tc-CDG-tetrac with human umbilical vein endothelial (HUVE) cells at 37℃ for 6 h. The cell binding of the radioligand increased from 100% at 0.5 h to 293.7% at 6 h in a time-dependent manner. For blocking study, the cells were incubated with the radioligand in the presence of either tetrac (20 μM) or cRGDyK (20 μM) at 37℃ for 4 h. The results demonstrated that the cell binding of the radioligand was inhibited by tetrac (19.1%) or cRGDyK (35.6%), indicating specific binding of the radioligand to integrin α_vβ₃. Thus, this study suggests that [^99mTc]Tc-CDG-tetrac may be a potential radioligand for tumor angiogenesis imaging.

• Journal of radiological science and technology
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• v.43 no.2
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• pp.97-103
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• 2020

This study was conducted by SPECT test at the Department of Nuclear Medicine at Daegu P Hospital from June 1 to October 31, 2019. A 3-way injection material was mounted among inpatients, and a syringe that was administered with radiopharmaceuticals using a ^99mTc labeled compound was secured. We tried to find a way to calculate the dose rate of each radiopharmaceutical and increase the dose rate. As a result of measuring the radioactivity of radio-pharmaceuticals using ^99mTc, the average dose rate of 60 syringes of all 6 radiopharmaceuticals was 93.26±7.34%, and the average dose rate of ^99mTc-DMSA was 77.72%, 15.54% lower than the total. As a way to increase the dosing rate, the average dose rate diluted twice with the remaining amount of syringe after administration using normal saline increased to 95.37±6.99%, and the average dose rate diluted three times increased to 96.32±6.86%. The corresponding sample t-test to compare the pre- and post-dose rates at 1 dilution and 2 and 3 dilutions. As a result of the dilution and 2 dilutions, the probability of significance was 0.013, which was significantly higher than the dilution(p<0.05). The probability of significance for dilution 1 and dilution 3 was 0.016, which was significantly higher than in one dilution(p<0.05). The sum of the average dose rate using the experimental 3-way line was the highest with 98.85±1.42% of ^99mTc, ^99mTc-ECD 98.82±1.26%, ^99mTc-Mebrofenin 98.82 ± 1.16%, ^99mTc-HDP 98.74 ± 1.91%, ^99mTc -MIBI was 98.69 ± 1.48%, and ^99mTc-DMSA was the lowest with 86.47 ± 4.74%. When the number of dilutions was 5 times using 0.5 cc of normal saline and when the number of dilutions was 5 times using 1 cc of normal saline, when the number of dilutions was 5 times using 0.5 cc of normal saline and 1 cc of nomal saline When the number of dilutions was 5 times and the syringe volume was 0.5 cc, there was a statistically significant difference (p<0.05). There was a statistically significant difference when the number of dilutions was 5 times using 1 cc of nomal saline and the number of dilutions was 5 times using 1 cc of normal saline, and the syringe volume was 0.5 cc (p<0.05).

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.5 no.1
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• pp.3-10
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• 2019

The activities per volume of $^{188}Re$ and $^{99m}Tc$ from their generators are dependent on the specific activity of their mother nuclides $^{188}W$ and $^{99}Mo$ respectively. After a particular lapse of time, the eluted RI activity is exponentially reduced and thus cannot satisfy the needs of clinical application. The purpose of this study is to develop a $^{188}Re$ and $^{99m}Tc$ concentration device with a compact size that can extend the period of use as well as conveniently concentrate the RI. We designed the concentration module by including two-different check valves that do not required any manual on-off operations. In these concentration process, cation exchange resin embedded with Ag and anion exchange resins were used. After completing the concentrating step, the recovering yield was identified to be more than 93% for $^{188}Re$ generators and 88% for $^{99m}Tc$ generators. Moreover, all these procedures were done within 5 min.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.4 no.2
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• pp.73-79
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• 2018

In our previous study, tricarbonyl $^{99m}Tc$-labeled TSPO-binding ligand, named $^{99m}Tc$-CB256, having positively charge (+1) was investigated but did not show promising results in in vivo environment despite of a nanomolar binding affinity for TSPO. Because the overall positively charge of $^{99m}Tc$-CB256 would likely interrupt its target protein uptake, we herein designed the neutral tricarbonyl-$^{99m}Tc$ labeled TSPO-binding ligand ($^{99m}Tc$-CB257, 1). $^{99m}Tc$-CB257 was prepared by the facile incorporation of the $[^{99m}Tc(CO)_3]^+$ into a N-(hydroxycarbonylmethyl)-2-picoly moiety in CB257. The radiochemical yield of $^{99m}Tc$-CB257 after HPLC purification was $54.1{\pm}2.4%$ (decay corrected, n = 3). The authentic Re-CB257 (2) was synthesized by using $(NEt_4)_2[Re(CO)_3Br_3]$ in 69.0% yield. The binding affinity of 2 for TSPO was measured in leukocyte and showed approximately 280 times higher than that observed for the positively charged (+1) ligand, Re-CB256 ($K_i=0.57{\pm}0.06nM$ versus $159.3{\pm}8.7nM$, respectively). Our results indicated that 1 can be considered potentially as a new SPECT radiotracer for TSPO-rich cancer and provides the foundation for further in vivo evaluation related with abnormal TSPO-overexpression environments.

• Journal of the Korea Convergence Society
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• v.8 no.8
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• pp.147-154
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• 2017

The purpose of this study is to calculate and compare administered activities(MBq) and effective dose(mSv) of the various pediatric dose formulas of pediatric nuclear medicine and to provide base data for the criteria of the optimal administered activities. This study compares dosages and effective doses of 5 types of pediatric dose formulas(Clark rule, Area rule, Webster rule, Young rule, Solomon(Fried) rule) based on the dosage for adults of 2 types of radiopharmaceuticals($^{99m}Tc$-MDP, $^{99m}Tc$-Pertechnetate). The administered activities in adults, which is the criteria for calculating the Pediatric administered activities, used the value from the 'Nuclear Medicine' written by J-G Jeong & M-Ch Lee. and the administered activities by the radioactivity per effective dose(mSv/MBq) of the radiopharmaceuticals for calculating the effective dose used the value from ICRP 80 and the UNSCEAR 2008 Report. As a result of the study, the output of Young rule is the lowest, and its difference between other formulas is from minimum 1.7 times to maximum 3,4 times. The difference between administered activities of $^{99m}Tc$-MDP is maximum 309.9MBq and the effective dose is 3.76mSv. $^{99m}Tc$-Pertechnetate showed the figure at the maximum 154.9MBq and the effective dose has a difference of 5.50mSv. Since the pediatric dose formulas differ not only in administered activities but also in effective doses, the optimal administered activities have to be developed for optimization of medical radiation.