• 대한수의학회지
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• 제44권1호
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• pp.15-21
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• 2004

This paper describes the development of $^{99m}Tc$ tricarbonyl cysteine as potential renal function diagnostic radiopharmaceutical and evaluation of its biological characteristics using experimental animals. l-Cysteine was labeled efficiently with $^{99m}Tc$ tricarbonyl precursor $([^{99m}Tc(CO)_3(H_2O)_3)]^{+})$ under 30 min heating at ${75^{\circ}C}$. Labeling yield and stability were analyzed by high performance liquid chromatography (HPLC). The biodistribution property of $^{99m}Tc$ tricarbonyl cysteine in mice and its dynamic imaging profiles in rabbits were carried out. To investigate the excretion mechanism of $^{99m}Tc$ tricarbonyl cysteine, tubular transport inhibition test with probenecid was adopted. $^{99m}Tc$ tricarbonyl cysteine was obtained with a high labeling yield under the moderate condition. The results of biodistribution experiments of $^{99m}Tc$ tricarbonyl cysteine in ICR mice at 3 and 90 min provided that $^{99m}Tc$ tricarbonyl cysteine was very highly accumulated in the kidney and bladder, thereby almost 99% of $^{99m}Tc$ tricarbonyl cysteine was excreted within 90 min post injection. The same results were confirmed by the whole body dynamic images for 30 minutes and static images in rabbits at given time intervals after injection. Renogram of $^{99m}Tc$ tricarbonyl cysteine in rabbits showed that its $T_{max}$ and $T_{1/2}$ of $^{99m}Tc$ tricarbonyl cysteine were $2.33{\pm}0.56$ and $4.30{\pm}0.79$ min, respectively. The $T_{max}$ of $^{99m}Tc$ tricarbonyl cysteine with probenecid pretreatment was $2.30{\pm}0.17$ min, whereas $T_{1/2}$ of that with probenecid pretreatment was $17.0{\pm}32.47$ min. $T_{1/2}$ of $^{99m}Tc$ tricarbonyl cysteine with probenecid pretreatment was significantly different, as compared to the result without probenecid (p<0.0001). The results showed that the excretion of $^{99m}Tc$ tricarbonyl cysteine was extremely affected by probenecid. Therefore, $^{99m}Tc$ tricarbonyl cysteine was rapidly excreted from the kidney principally by the tubular secretion.

• 대한핵의학회지
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• 제30권4호
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• pp.484-492
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• 1996

허혈성 뇌 병변에서 $^{99m}Tc$-glucarate의 섭취에 관한 연구를 하기 위하여 중뇌동맥 폐쇄 쥐 뇌허혈 모델을 재관류한 군과 하지 않은 군으로 나누어 만들었다. $^{99m}Tc$-glucarate와 [$^{18}F$]FDG를 연속적으로 투여하여 그 분포 양상을 이중 자가방사촬영법으로 관찰하였다. 조직의 괴사 여부를 알기 위하여 TTC 염색도 실시하여 동일한 뇌표본에 대하여 3가지의 영상을 동시에 얻을 수가 있었다. 얻은 영상으로 섭취 또는 비섭취정도를 보아 0점에서 3점까지 점수를 매겨 합하여 비교하였다. 수술한 쥐들 18마리 중 10마리가 신경학적 증상을 보이면서 살아남아 실험대상이 되었다. TTC 염색으로 확인한 경색크기는 재관류하지 않은 군이 컸다. [$^{18}F$]FDG 섭취양상은 TTC 염색과 거의 비슷하였다. 다만 일부에서 TTC 염색되는 곳에 [$^{18}F$]FDG 가 중간정도로 섭취되는 곳이 있었고 TTC 염색되지 않는 곳에 [$^{18}F$]FDG가 중간정도 섭취되는 곳이 있었다. TTC로 염색된 부위에는 $^{99m}Tc$-glucarate가 섭취되지 않았다. TTC로 염색되지 않는 곳에 일부분 $^{99m}Tc$-glucarate가 섭취되었다. TTC와 [$^{18}F$]FDG가 염색되거나 섭취되지 않는 곳에 $^{99m}Tc$-glucarate가 섭취되지 않는 곳이 있었다. 그러나 [$^{18}F$]FDG의 중간 정도의 섭취나 [$^{18}F$]FDG와 TTC사이에 부합하지 않는 곳 등과 $^{99m}Tc$-glucarate 섭취와 대응시키기 어려웠다 $^{99m}Tc$-glucarate가 재관류 군에서 더 넓고 많이 섭취되었다. 결론적으로 $^{99m}Tc$-glucarate는 비생존 허혈조직에만 섭취되는데 관류재개통에 따라 다양하게 섭취되었고 재관류모델에 더 많이 넓게 섭취되었다. 중뇌동맥폐색 및 재관류 모델로 $^{99m}Tc,\;^{18}F$ 및 TTC 동시영상을 얻어 생존능과 포도당대사의 부합 비부합 여부를 밝히고 그 의의를 조사한 후 $^{99m}Tc$-glucarate섭취와 상관을 조사하면 $^{99m}Tc$-glucarate섭취의 의의를 밝힐 수 있을 것으로 본다.

• 핵의학기술
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• 제20권2호
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• pp.36-41
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• 2016

1. 목적 현재 감시림프절 검사에는 $^{99m}Tc-Phytate$만 사용한다. 만약 일시적으로 공급이 중단된다면 대체 가능한 방사성의약품이 없는 실정이다. 본 연구에서는 감시림프절 검사의 성공요소 중 방사성의약품의 입자 크기에 중점을 두어 핵의학 검사에 사용되는 방사성의약품들의 입자크기를 측정해보고 감시림프절 검사 시 $^{99m}Tc-Phytate$를 대체할 수 있는 방사성의약품을 찾아보고자 하였다. 2. 방법 Zetasizer Nano ZS90 (Malvern, UK)를 통하여 체내검사에 이용되는 Phytate, MAG3, DPD, DMSA, MAA, DTPA, HDP의 입자크기를 분석하였다. 동물실험은 9주령의 백서 6마리를 사용하여 각각 3마리씩 $^{99m}Tc-Phytate$를 사용한 대조군과 감시림프절 검사 시 유용하다고 알려진 입자크기를 갖는 $^{99m}Tc-MAG3$, $^{99m}Tc-DPD$와 $^{99m}Tc-DMSA$를 사용한 실험군을 설정 하였다. 백서의 발등에 11.1 MBq ($300{\mu}Ci$)을 인슐린 주사기를 이용하여 피하주사 하고, 동적영상과 정적지연영상을 획득한 후 육안으로 서혜부 림프절을 관찰하였다. 3. 결과 나노입자 분석기를 통하여 측정한 입자크기는 각각 Phytate 105~255 nm ($81.9{\pm}23%$), MAG3 91~255 nm ($98.7{\pm}17%$), DPD 105~342 nm ($77.3{\pm}11%$), DMSA 164~342 nm ($99.2{\pm}35%$), MAA 1281~2305 nm($90.6{\pm}82%$), DTPA 342~1106 nm ($79.4{\pm}28%$), HDP 295~955 nm ($94{\pm}33%$)로 나타났다. $^{99m}Tc-Phytate$를 사용한 대조군은 모든 실험에서 서혜부 림프절을 육안으로 확인 할 수 있었다. $^{99m}Tc-Phytate$와 가장 유사한 크기의 $^{99m}Tc-MAG3$는 서혜부 림프절에 저류하지 않고 빠르게 통과하였고, $^{99m}Tc-DPD$와 $^{99m}Tc-DMSA$를 이용한 실험에서는 서혜부 림프절에 대조군과 비슷하게 저류되어 림프절 관찰이 용이하였다. 결론: 본 실험을 통해서 핵의학 체내검사에 사용되는 방사성의약품들의 입자크기 분포를 확인하였다. $^{99m}Tc-MAG3$는 $^{99m}Tc-Phytate$와 가장 유사한 입자크기를 가지고 있으나 동물실험에서는 서혜부 림프절이 관찰되지 않고 빠르게 신장을 통해 배출되었다. 반면에 $^{99m}Tc-DPD$나 $^{99m}Tc-DMSA$의 경우 유사시 대체 방사성의 약품으로 사용 될 수 있을 것으로 생각된다.

• 대한핵의학회지
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• 제37권2호
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• pp.135-136
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• 2003

A 43-year-old woman with diabetic nephropathy underwent a Tc-99m MAG3 renal scintigraphy for the evaluation of renal function. Posterior images at 60 minutes demonstrated a migration of radiotracer activity beyond the lower pole of the left kidney, which might be incorrectly interpreted as urine leaks. However, the increased activities were moving along the bowel lumens over time. Another ring-like radioactivity was also seen in the suprasplenic region, and increased with time. These radioactivities were in the gastric fundus and gastrointestinal tract and caused by free Tc-99m pertechnetate.

• 대한핵의학회지
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• 제20권2호
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• pp.53-59
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• 1986

Radionuclide angiography of the liver and spleen with rapid bolus injection of 5 mCi of $^{99m}Tc-Sn-phytate$ was performed for evaluation of dynamic flow change of the liver in 5 normal subjects and 11 patients with diffuse hepatocellular diseases. And quantification of hepatic arterial index (HAI) was generated from those TACs of the liver and compared with HAI generated from hepatic TAC with injection of $^{99m}Tc-TcO_4^-$ as previously reported method by former investigators, 67 patients with diffuse hepatocellular diseases undergoing hepatic scintigraphy were also evaluated by 2 minutes-hepatosplenic scintiangiography with 5 mCi of $^{99m}Tc-phytate$ and followed injection of 7 mCi of $^{99m}Tc-TcO_4^-$. Those heaptic and splenic TACs were analysed and compared with HAIs of 99m Tc-phytate for evaluation of relative change (%) of count at 30 seconds and 1 minuite after peaks of rapid influx phase to the peaks (100%) in T ACs of $^{99m}Tc-phytate$ and at 1 minuite and 3 minuites after in 5 minuite-TAC of $^{99m}Tc-TcO_4^-$. Correlation between HAIs with $^{99m}Tc-phytate$ and $^{99m}Tc-TcO_4^-$ was highly significant (R=0,984, P=0), and there was most significant and useful correlation (R=0,708, p<0.0001) between HAI and splenic TAC generated by $^{99m}Tc-phytate$.

• Nuclear Engineering and Technology
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• 제34권2호
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• pp.146-153
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• 2002

To radiolabel bioactive molecules, we synthesized $^{99m}$Tc-tricarbonyl precursor, [$^{99m}$Tc(CO)$_3$($H_2O$)$_3$]$^{+}$ with a low oxidation state ( I ). The [$^{99m}$Tc(CO)$_3$($H_2O$)$_3$]$^{+}$ was prepared by low pressure carbonylation (1 atm of CO) of [$^{99m}$Tc $O_4$)]$^{[-10]}$ in the presence of NaB $H_4$ resulting in higher than 98% of labeling yield and stability up to 8 hrs. We evaluated the characteristics of $^{99m}$Tc- tricarbonyl labeled bioactive molecules by carrying out in vitro and in vitro study. Prepared [$^{99m}$Tc(CO)$_3$($H_2O$)$_3$]$^{+}$ was then reacted with some ligands of significance in modem diagnostic nuclear medicine and some amino acids. Labeling yields were checked by HPLC and found to be usually high, excluding $^{99m}$Tc-tricarbonyl-MDP, -EDTMP and -mIBG. And the biodistribution properties of $^{99m}$Tc-tricarbonyl complexes applied in rabbit showed different appearance comparing with that of the $^{99m}$Tc-labeling by conventional means. From these results, we conclude that [$^{99m}$Tc(CO)$_3$($H_2O$)$_3$]$^{+}$ is a potential precursor for development of radiopharmaceuticals, especially for labeling of biomolecules.

• Nuclear Medicine and Molecular Imaging
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• 제40권3호
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• pp.177-185
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• 2006

목적 : 본 연구의 목적은 $^{99m}Tc$-방사성표지 트렌스페린 ($^{99m}Tc$-transferrin)을 개발하여 감염/염증병소의 진단에 이용할 수 있는지 알아보고, 이를 $^{67}Ga$-Citrate 영상과 비교하고자 하였다. 대상 및 방법 : Succinimidyl 6-hydrazino-nicotinate hydrochloride -chitosan -transferrin (Transferrin)을 합성하고, 여기에 $^{99m}Tc$ 방사성 표지를 시행하였다. $^{99m}Tc$-transferrin의 방사성표지효율은 표지 후 10분, 30분, 1시간, 2시간, 4시간, 8시간에 측정하였다. 포도상구균(ATCC 25923, $2{\times}10^8$ colony forming unite, 0.2 ml)을 접종한 쥐농양모델에서 $^{99m}Tc$-transferrin과 $^{67}Ga$-citrate의 생체내 분포를 평가하고 영상 검사를 실시하였다. 결과: 질량분석계를 이용하여 Transferrin이 성공적으로 제조되었음을 알 수 있었다. $^{99m}Tc$-transferrin의 방사성표지효율은 10분, 30분, 1시간, 2시간, 4시간, 8시간에 각각 $96.2{\pm}0.7%,\;96.4{\pm}0.5%,\;96.6{\pm}1.0%,\;96.9{\pm}0.5%,\;97.0{\pm}0.7%\;and\;95.5{\pm}0.7%$ 이었다. $^{99m}Tc$-transferrin의 단위섭취량은 감염병소에서 $0.18{\pm}0.01\;and\;0.18{\pm}0.01$, 정상근육에서 $0.05{\pm}0.01\;and\;0.04{\pm}0.01$이었고, 감염병소 대 정상근육 섭취비는 30분과 3시간에 각각 $3.7{\pm}0.6\;and\;4.7{\pm}0.4$이었다. $^{99m}Tc$-transferrin 영상에서 10분, 30분, 1시간, 2시간, 4시간 그리고 10시간에서의 병소/배후방사능비는 각각 $2.18{\pm}0.03,\;2.56{\pm}0.11,\;3.08{\pm}0.18,\;3.77{\pm}0.17,\;4.70{\pm}0.45$ 그리고 $5.59{\pm}0.40$이었고, $^{67}Ga$-citrate의 경우 2시간, 24시간, 48시간에 $3.06{\pm}0.84,\;4.12{\pm}0.54\;4.55{\pm}0.74 $이었다. 결론 : Transferrin에 $^{99m}Tc$을 이용한 방사성표지가 성공적으로 이루어졌고, $^{99m}Tc$-transferrin의 표지효율은 8시간까지 95% 이상의 안정된 방사성표지효율을 보였다. $^{99m}Tc$-transferrin을 이용한 감염영상을 성공적으로 얻을 수 있었으며, $^{67}Ga$-citrate 영상과 비교하여 더 빠른 시간 안에 우수한 영상을 얻을 수 있었다. 그러므로 $^{99m}Tc$-transierrin이 감염 병소의 영상진단에 사용될 수 있을 것으로 기대된다.

• 대한핵의학회지
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• 제37권3호
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• pp.202-205
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• 2003

A 10 days old male infant with congenital megacalyces and megaureter, diagnosed by prenatal ultrasonographic screening, underwent Tc-99m DTPA renal scan for evaluation of urinary tract patency, Tc-99m DMSA scan for evaluation of renal cortical damage. He also underwent intravenous urography(IVU) and renal ultrasonography. Tc-99m DTPA renal scan demonstrates intense tracer accumulation in enlarged both renal pelvocalyses and ureters, which rapidly washout without diuretics administration. Tc-99m DMSA renal cortical scan shows no remarkable photon defect in both renal cortices and visible tracer uptake in both megaureter areas. Ultasonographic and IVU studios show enlarged both renal calyses and bullously dilated ureters, but no dilatation in renal pelvis. Follow up Tc-99m DTPA renal scan, peformed at one year later, also reveals intense tracer accumulation in enlarged both urinary tracts which rapidly washout without diuretics, and shows no significant change compare to the previous Tc-99m DTPA renal scan. Urinary tract obstruction and renal cortical damage can be easily evaluated with Tc-99m DTPA and Tc-99m DMSA scans in patiens with megacalyces and megaureter.

• Toxicological Research
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• 제28권4호
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• pp.235-240
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• 2012

$^{99m}Tc$ tricarbonyl glycine monomers, trimers, and pentamers were synthesized and evaluated for their radiolabeling and in vivo distribution characteristics. We synthesized a $^{99m}Tc$-tricarbonyl precursor with a low oxidation state (I). $^{99m}Tc(CO)_3(H_2O)_3^+$ was then made to react with monomeric and oligomeric glycine for the development of bifunctional chelating sequences for biomolecules. Labeling yields of $^{99m}Tc$-tricarbonyl glycine monomers and oligomers were checked by high-performance liquid chromatography. The labeling yields of $^{99m}Tc$-tricarbonyl glycine and glycine oligomers were more than 95%. We evaluated the characteristics of $^{99m}Tc$-tricarbonyl glycine oligomers by carrying out a lipophilicity test and an imaging study. The octanol-water partition coefficient of $^{99m}Tc$ tricarbonyl glycine oligomers indicated hydrophilic properties. Single-photon emission computed tomography imaging of $^{99m}Tc$-tricarbonyl glycine oligomers showed rapid renal excretion through the kidneys with a low uptake in the liver, especially of $^{99m}Tc$ tricarbonyl triglycine. Furthermore, we verified that the addition of triglycine to prototype biomolecules (AGRGDS and RRPYIL) results in the improvement of radiolabeling yield. From these results, we conclude that triglycine has good characteristics for use as a bifunctional chelating sequence for a $^{99m}Tc$-tricarbonyl-based biomolecular imaging probe.

• Journal of Microbiology and Biotechnology
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• 제18권9호
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• pp.1599-1605
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• 2008

Biodistribution and lymphoscintigraphy of cyclosporine A (CyA) and technetium-99m ($^{99m}Tc$) were studied using ${^99m}Tc$-labeled dextran acetate (DxA) including CyA. DxA particles were prepared from dextran with acetic anhydride, and CyA was loaded into them. Lymphatic delivery of ${^99m}Tc$-labeled DxA particles containing CyA was evaluated after subcutaneous injection into the foot pad of rats and compared with those of ${^99m}Tc$-labeled human serum albumin (HSA). The labeling efficiency of CyA-loaded ${^99m}Tc$-DxA particles was about 95% at 30 min. The labeling efficiency maintained stably above 80% for 12 h. The percent injected dose (%ID) of CyA-loaded ${^99m}Tc$-DxA was similar to that of ${^99m}Tc$-HSA at the inguinal lymph node after 40 min. The CyA-loaded ${^99m}Tc$-DxA could be as well distributed as ${^99m}Tc$-HSA through the lymph node. The DxA particles could steadily distribute the CyA as well as the ${^99m}Tc$ radiolabeling through the lymph node.