• The Korean Journal of Nuclear Medicine
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• v.27 no.2
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• pp.270-276
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• 1993

$Technetium-^{99m}$ labeling method using bifunctional chelating agent cyclic DTPA has been evaluated with human polyclonal nonspecific IgG. IgG was conjugated with cyclic DTPA with various molar ratio. Reduction of $^{99m}Tc$ was done with $Na_2S_2O_4$ with various molar excess. Labeling efficiency and identification of polymer was confirmed with HPLC using TSK4000 SW column. Polymer was purified with 100 cm Sepharose 6LB column. Cultured $1{\times}10^9$ Staphylococcus aureus were injected into rat thigh 24 hours later labeled IgG was injected, and in vivo distribution was observed 4 and 24 hours thereafter. Reduction of $^{99m}Tc$ was optimal with the 10000-50000 times molar excess of $Na_2S_2O_4$. Polymer formation increased with increasing mloar excess of cyclic DTPA to IgG. Three step labeling-labeling DTPA conjugated IgG after reduction of $^{99m}Tc$-made more polymer than two two step labeling-simultaneous mixing DTPA conjugated IgG, $^{99m}Tc$ and $Na_2S_2O_4$. $^{99m}Tc$ blood clearance and lower uptake in the abscess and other organs. IgG conjugated with 200 times molar excess of cyclic DTPA showed slower blood clearance with 200 times molar excess of cyclic DTPA showed slower blood clearance than that of 200 times molar excess of cyclic DTPA showed slower blood clearance than that of 20 times molar excess. In the $^{99m}Tc$ labeling of IgG with cyclic DTPA for the immunoscintigraphy, obtimal labeling condition should be chosen, and effect of the $^{99m}Tc$ labeled IgG polymer should be considered.

• Journal of the Korean Chemical Society
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• v.33 no.5
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• pp.484-495
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• 1989

Reactions of $(Et_4N)_2[MoOCl_5]$ with multidentate ligands containing nitrogen or/and oxygen donor atom (EDTA, DTPA, IDA, CyDTA, OX) produce a series of binuclear molybdate (V) complexes. The prepared Mo (V) complexes has been identified by Elemental Analysis, Infrared Spectra, Proton Magnetic Resonance Spectra, and Electronic Spectra. The electrochemical reduction mechanism has been studied by Cyclic voltammetry, Controlled Potential Coulometry, and Spectrophotometry in pH 3.571-10.375 acetate, borate, phosphate/sodium hydroxide, phosphate, ammonium/ammonia buffers. The cyclic voltammogram of the Mo-EDTA, DTPA, IDA, CyDTA complexes at pH < ca. 6.00 have shown two reduction waves. The first reduction wave shows two electron process and the second reduction wave shows two electron process. The cyclic voltammogram of the Mo-EDTA, DTPA, IDA, CyDTA complexes at pH < ca. 8.00 has shown one reduction wave. This reduction wave show four electron process. The cyclic voltammogram of the Mo-OX complex at pH < ca. 7.2 has shown one reduction wave. This reduction wave show four electron process.

• The Korean Journal of Nuclear Medicine
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• v.37 no.6
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• pp.402-417
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• 2003

Purpose: To evaluate the use of monoclonal antibody (MoAb) as a carrier of the receptor-binding ligand the receptor mediated uptake into liver and subsequent metabolism of $^{111}In-labeled$ galactosylated MoAb-chelator conjugates were investigated and compared with those of $^{111}In$ labeled MoAb. Materials and Methods : T101 MoAb, $IgG_2$ against human lymphocytic leukemic cell, conjugated with cyclic DTPA dianhydride (DTPA) or 2-p-isothiocyanatobenzyl-6-methyl-DTPA (1B4M) was galactosylated with 2-imino-2-methoxyethyl-1-thio-${\beta}$-D-galactose and then radiolabeled with $^{111}In$. Biodistribution and metabolism study was peformed with two $^{111}In-conjugates$ in mice and rats. Results: $^{111}In-labeled$ T101 and its galactosylated conjugates were taken to the liver by the time, mostly within 10 min. However DTPA conjugate was retained longer in the liver than the 1B4M conjugate (55% vs 20% of injected dose at 44 hr). During this time, the radiornetabolite of DTPA conjugate was excreted similarly into urine (24%) and feces (17%). The radiometabolite of 1B4M was excreted primarily into feces (68%) rather than urine (8%). Size exclusion HPLC analysis of the bile and supernatant of liver homogenate showed two peaks the first (35%) with the retention time (Rt) identical to IgG and the second (65%) with Rt similar to free $^{111}In$ at 3 hr post-injection for the 1B4M conjugate, indicating that the metabolite is rapidly excreted through the biliary system. in contrast to DTPA conjugate, the small $^{111}In-DTPA-like$ metabolite was the major radioindium component (90%) in the liver homogenate as early as 3 hour post-injection, but the cumulative radioindium activity in feces was only 17% at 44 hour, indicating that the metabolite from DTPA conjugate does not clear readily through the biliary tract. Conclusion: The galactosylation of the MoAb conjugates resulted in higher hepatocyte uptake and enhanced metabolism, compared to those without galactosylation. Metabolism of the MoAb-conjugates is different between compounds radiolabled with different chelators due to different characteristics of radiometabolites generated in the liver.

• Investigative Magnetic Resonance Imaging
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• v.4 no.1
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• pp.27-33
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• 2000

Purpose: To determine the electronic spin relaxation times, $T_{le}$, of three commercially available Gd-chelated MR contrast agents, Gd-DTPA, Gd-DTPA-BMA and Gd-DOTA, using Electron Paramagnetic Resonance(EPR) technique. Material and Methods: The paramagnetic MR contrast agents, Gd-DTFA(Magnevist) , Gd-DTFA-BMA(OMNISCAN) and Gd-DOTA(Dotarem), were used for this study, The EPR spectra of these contrast agents, which were prepared 2:1 methanol/water solution, were obtained at low temperatures, from $-160^{\circ}C~20^{\circ}C$. The glassy-state EPR spectra for these contrast agents were then fitted by the simulation spectra generated with different zero-field splitting (ZFS) parameters by a computer simulation program 'GEN', which generates the EPR powder spectrum using a given ZFS in $3{\times}3$ tensor. Finally, the spin relaxation times of the contrast agents were then determined from the $T_{2e}$, D, and E values of the best simulation spectra using the McLachlan's theory of average relaxation rate. Results: The electronic transverse spin relaxation times, $T_{2e}'s$, of Gd-DTPA, Gd-DTPA-BMA and Gd-DOTA were 0.113ns, 0.147ns and 1.81ns respectively. The g-values were 1.9737, 1.9735 and 1.9830 and the electronic spin relaxation times, $T_{1e}'s$, were 18.70ns, 33.40ns and $1.66{\mu}s$, respectively. Conclusion: The results of these studies reconfirm that the paramagnetic MR contrast agents with larger ZFS parameters should have shorter $T_{1e}'s$. Among three contrast agents used for this study, Gd-DOTA chelated with cyclic ligand structure shows better electronic property then the others with linear structure. Thus, it is concluded that the exact determination of ZFS parameters is the important factor in evaluating relaxation enhancement effect of the agents and in developing new contrast agents.