• Journal of Radiopharmaceuticals and Molecular Probes
• /
• v.1 no.1
• /
• pp.15-22
• /
• 2015

$^{18}F$-labeling reaction of bioactive molecule via click chemistry is widely used to produce $^{18}F$-labeled radiotracer in the field of radiopharmaceutical science and molecular imaging. In particular, bioorthogonal strain-promoted alkyne-azide cycloaddition (SPAAC) reaction has received much attention as an alternative ligation method for radiolabeling bioactive molecules such as peptides, DNA, proteins as well as nanoparticles. Moreover, SPAAC based pretargeting method could provide tumor images successfully on positron emission tomography system using nanoparticle such as mesoporous silica nanoparticles.

• Korean Journal of Environmental Biology
• /
• v.39 no.4
• /
• pp.550-558
• /
• 2021

In a radiotracer study, the bioaccumulation and efflux of metals in earthworms (Eisenia fetida) exposed to soil spiked with ZnO and Ag nanoparticles (AgNP) were compared to those exposed to soil spiked with ionic Zn and Ag. Additionally, the bioavailability and chemical mobility of nano- and ionic metals in the soil were estimated using the sequential extraction method and compared to the bioaccumulation factor(BAF). The BAF for ZnO (0.06) was 31 times lower than that for Zn ions (1.86), suggesting that ZnO was less bioavailable than the ionic form in contaminated soil. In contrast, the BAFs for two types of AgNPs coated with polyvinylpyrrolidone (0.12) or citrate (0.11) were comparable to those of ionic Ag (0.17). The sequential extraction of metals from the soil suggests that the chemically mobile fractions in the Zn ion treatment were higher(35%) than those (<20%) in the Ag ion treatment, which was consistent with the greater BAFs in the former than the latter. However, the chemical mobility in the ZnO treatments did not predict bioavailability. The efflux rates of Ag (3.2-3.8% d^-1) in the worms were 2-3×those(1.2-1.7% d^-1) for Zn.

• Journal of Korean Society of Coastal and Ocean Engineers
• /
• v.16 no.3
• /
• pp.162-170
• /
• 2004

On the basis of the radiotracer technology and the related equipments which have been developed for its industrial application through the nuclear long-term research project, a radiotracer study on sediment transport was carried out as a part of the development of the radiotracer technology for a coastal environment. The crystalline material doped with iridium having a similar composition and specific gravity as those of the bedload sand collected from the research area was produced by the oxide-route method. A radioisotope container was specially designed to inject the radiotracer from 1 m above the sea bedload without radioactive contamination during the transport from the nuclear reactor at KAERI. The position data from the DGPS and the radiation measurement data were collected concurrently and stored by means of the application software programmed with the LabVIEW of the National Instrument. The position data was reprocessed to represent the real position of the radiation probe under water and not that of the DGPS antenna on board. The time dependency of the spatial distribution of the sediment was studied in the area through three tracking measurements after the iridium glass was injected. This trial application showed the potential of the radiotracer technology as an important role for maintaining and developing the coastal environment in the future.

• The Korean Journal of Nuclear Medicine
• /
• v.38 no.4
• /
• pp.325-329
• /
• 2004

Purpose: Usefulness of mouse liver S9 fraction was evaluated for the measurement of the metabolites in the in vitro metabolism study of $^{18}F$-labeled radiotracers. Materials and Methods: Mouse liver S9 fraction was isolated at au early step in the course of microsome preparation. The in vitro metabolism studies were tarried out by incubating a mixture containing the radiotracer, S9 fraction and NADPH at $37^{\ciirc}C$, and an aliquot of the mixture was analyzed at the indicated time points by radio-TLC. Metabolic defluorination was further confirmed by the incubation with calcium phosphate, a bone mimic. Results: The radiotracer $[^{18}F]1$ underwent metabolic defluorination within 15 min, which was consistent with the results of the in vivo method and the in vitro method using microsome. Radiotracer $[^{18}F]2$ was metabolized to three metabolites including $4-[^{18}F]fluorobenzoic$ acid within 60 min. It is likely that the one of these metabolites at the origin of radio-TLC was identical with the one that obtained from the in vivo and in vitro (microsome) method. Compared with the in vitro method using microsome, the method using S9 fraction gave a similar pattern of the metabolites but with a different ratio, which can be explained by the presence of cytosol in the S9 fraction. Conclusion: These results suggest that the findings of the in vitro metabolism studies using S9 fraction can reflect the in vivo metabolism of novel radiotracers in the liver. Moreover, this method can be used as a tool to determine metabolic defluorination along with calcium phosphate absorption method.

• Bulletin of the Korean Chemical Society
• /
• v.20 no.9
• /
• pp.999-1004
• /
• 1999

Two compact sized globular proteins, β-lactoglobulin and α-lactalbumin were kinetically characterized at the aqueous solution surface with the measurement of surface pressure (π) and surface concentration (Γ) via a radiotracer method. The adsorption kinetics was of diffusion control at early times, the rates of increase of πand Γ being lower at longer times due to growing energy barrier. At low concentrations, an apparent time lag was observed in the evolution of π for β-lactoglobulin but not for α-lactalbumin which was shown to be due to the non-linear nature of the p- G relationship for the former. The area per molecule of an adsorbed β-lactoglobulin during adsorption was smaller than that for spread monolayer since β-lactoglobulin was not fully unfolded during the adsorption. For α-lactalbumin, however, no such difference in the molecular areas for adsorbed and spread monolayer was observed indicating thereby that α-lactalbumin unfolded much more rapidly (has looser tertiary structure) than β-lactoglobulin. Surface excess concentrations of α-lactalbumin was found to evolve in two steps possibly due to the change in the orientation of the adsorbed protein from a side-on to an end-on orientation.

• Journal of Radiopharmaceuticals and Molecular Probes
• /
• v.4 no.2
• /
• pp.51-56
• /
• 2018

Azeotropic drying process is routinely applied to enhance nucleophilicity of $[^{18}F]$fluoride ion during the nucleophilic production of PET radiotracers; however, the drying process requires usually 15-25 min. Due to the high demand of employing fluorine-18 ($t_{1/2}=109.8min$) in PET radiopharmaceutical production, several research groups have focused on the method development, obviating tedious removal process of the residual target water ($[^{18}O]H_2O$) for $[^{18}F]$fluoride ion complex to be used in radiofluorination. Some development in radiofluorination in a mixed organic solvent system was demonstrated with various aliphatic substrates, but only kryptand as a phase transfer agent was utilized in the reported method. Here, we extend to investigate the development scope of applicability with basic alkyl ammonium salt as a phase transfer agent through the extensive elution efficiency study and radiofluorination outcome for aliphatic radiofluorination.

• Progress in Medical Physics
• /
• v.22 no.4
• /
• pp.172-177
• /
• 2011

The purpose of this study was to analyze $^{68}Ga$-BAPEN dynamic PET image in rat myocardium to evaluate potential of this radiotracer as a perfusion imaging agent. Animal PET/CT scan was done in 9 rats during 120 minutes. Especially we synthesized $^{68}Ga$-BAPEN with kit which is simple and low cost method. PET images showed the in vivo dynamic distribution of $^{68}Ga$-BAPEN in the chest region of rats. Initially $^{68}Ga$-BAPEN PET images showed aorta and liver activities and a few minutes later, $^{68}Ga$-BAPEN moved to myocardium. Regions of interest were drawn on myocardium, liver, lung and blood pool. Time-activity curves showed significant uptake of $^{68}Ga$-BAPEN in myocardium. The contrast ratios of myocardial to blood pool, lung and liver at 60 minutes after injection were 1.66, 2.82 and 0.60. To estimate accurate kinetic parameters, 60 minutes after injection was required to PET scan as myocardium image contrast ratios reached to constant values. As a result, $^{68}Ga$-BAPEN would be suitable radiotracer for PET which can applied to diagnosis of myocardial perfusion diseases after further preclinical and clinical investigations.

• Journal of Radiopharmaceuticals and Molecular Probes
• /
• v.3 no.1
• /
• pp.3-14
• /
• 2017

Nucleophilic aromatic fluorination has been one of the most explored methods in fluorin-18 based radiochemistry. Unlike electrophilic $[^{18}F]$fluorination methods, no-carrier-added nucleophilic radiofluorination with cyclotron-produced $[^{18}F]$fluoride ion offers better specific radioactivity which is essential aspect to obtain good quality images from positron emission tomography. Contrary to amenable aliphatic radiofluorination, the development of reliable aromatic $[^{18}F]$fluorination methods has been pursued by many research groups; however, no viable method has yet been established. Recently, hypervalent iodine compound draws increasing attention as versatile radiolabeling precursor for various $[^{18}F]$fluoroarenes, since it bears the capacity to introduce fluorine-18 either on electron-deficient or electron-rich aryl ring with enhanced regiospecificity. Other classes of hypervalent iodine congeners often utilized in radiochemistry are iodylarenes, iodonium ylides, and spirocyclic iodonium ylides. Recently developed spirocyclic iodonium ylides have already been avidly employed to provide various $[^{18}F]$aryl fluorides with high labeling efficiency. This metal-free protocol would afford efficient routes, replacing the traditional approaches to $[^{18}F]$fluoroarenes, from prosthetic labeling synthons to complex PET radiotracers.

• ALGAE
• /
• v.20 no.2
• /
• pp.157-166
• /
• 2005

Uptake kinetics of Cd and Zn by leaves and rhizome of the seagrass Zostera marina were examined in controlled laboratory radiotracer experiments. Subsequently, acute toxicity of Cd, Cu and TBT on photosynthetic quantum yield (ΔF/Fm’ of Z. marina were determined, and the differential sensitivities of rapid light curve (RLC) to those harmful substances were also compared. All measurements on photosynthetic activity were determined by chlorophyll a fluorescence method using pulse amplitude modulation (PAM). Metal uptake by Z. marina was saturated with increasing exposure time in leaves and rhizomes. Uptake of Zn by Z. marina was faster than that of Cd. Metal uptake rates in Z. marina decreased with the increase of dissolved metal concentrations and also with the increase of biomass. The adverse effect of TBT on effective quantum yield was stronger than other pollutants. Average acute toxicity on the RLC of the seagrass exposed to TBT and two heavy metals (Cd and Cu) was going to decrease as follows: TBT > Cd > Cu. Our preliminary results in this study suggested that Z. marina potentially can be used as a biomonitor of harmful substances contamination in coastal waters.

• Nuclear Medicine and Molecular Imaging
• /
• v.43 no.1
• /
• pp.1-9
• /
• 2009

As many new drug substances contained various aromatic rings and fluorine attached to an electron rich aromatic ring or on the meta-position, a strategy towards improvement in aromatic fluorination of these compounds is highly desirable. The introduction of fluorine-18 onto aromatic rings showed in the limited condition containing electron withdrawing group (EWG) on the para- or ortho-position to get reasonable radiochemical yield so far. No-carrier added (NCA) [$^{18}F$]fluoroarene syntheses by iodonium salts recently reported that has the potential to greatly increase the yield in systems or positions that normally not reactive enough to give sufficient yields in simple model reaction. This review describes the methodological approach towards effective aromatic fluorination by diaryliodonium salts and future prospects in an application of novel PET radiotracer.