• Title/Summary/Keyword: Radioactive iodine

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Radiosynthesis of 125I-labeled 2-cyanobenzothiazole: A new prosthetic group for efficient radioiodination reaction

  • Mushtaq, Sajid;Choi, Dae Seong;Jeon, Jongho
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.3 no.1
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    • pp.44-51
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    • 2017
  • Herein we report an efficient radiolabeling method based on a rapid condensation reaction between N-terminal cysteine and 2-cyanobenzothiazole (CBT). Radioiodination of 2-cyano-6-hydroxybenzothiazole 2 was carried out using chloramine-T to give $^{125}I$-labeled CBT ([$^{125}I$]1) with a high radiochemical yield ($90{\pm}6%$ isolated yield, n=3) and radiochemical purity (>99%). To evaluate the radiolabeling efficiency of $^{125}I$-labeled CBT, model compounds, L-cysteine and N-terminal cysteine conjugated cRGD peptide were reacted with [$^{125}I$]1 under mild conditions. The radiolabeling reactions rapidly provided the $^{125}I$-labeled products [$^{125}I$]5 and [$^{125}I$]6 with excellent radiochemical yields and radiochemical purity. Therefore, we demonstrate that [$^{125}I$]1 will be a useful prosthetic group for radioactive iodine labeling of N-terminal cysteine bearing biomolecules.

Synthesis of 125I-labeled tetrazine for efficient radiolabeling of human serum albumin

  • Shim, Ha Eun;Jeon, Jongho
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.3 no.2
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    • pp.98-102
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    • 2017
  • We demonstrate a detail protocol for the radiosynthesis of a $^{125}I-labeled$ tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctene-group conjugated human serum albumin (3) using inverse-electron-demand Diels-Alder reaction. Radioiodination of the stannylated precursor (2) was carried out by using [$^{125}I$]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I-labeled$ azide ([$^{125}I$]1) was obtained with high radiochemical yield ($65{\pm}8%$, n = 5) and excellent radiochemical purity (>99%). Inverse-electron-demand Diels-Alder reaction between ([$^{125}I$]1) and 3 gave the $^{125}I-labeled$ human serum albumin ([$^{125}I$]4) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly indicate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.

A Case of Occult Papillary Carcinoma of Thyroid, Invaded Trachea and Esophagus (기관지 내시경에 의해 진단된 기관과 식도를 침범한 갑상선 잠재성 유두암 1예)

  • Cho, Deok-Su;Ahn, Byung-Yi;Lee, Deok-Su;Han, Dong-Ho;Kim, Sang-Young;Kim, Kwi-Wan
    • Tuberculosis and Respiratory Diseases
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    • v.44 no.5
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    • pp.1125-1131
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    • 1997
  • Occult papillary adenocarcinoma of the thyroid is known to be indolent, slow metastatic, and has a good prognosis. Occult thyroid carcinoma presenting as a blood-borne metastasis without obvious cervical lymph node involvement is extremely rare. A 65-year-old male patient was visited for hoarseness, dysphagia, and shortness of breath. Bronchoscopy with biopsy revealed a papillary carcinoma of thyroid by immunohistochemical staining. Head & neck CT revealed that involving both the upper esophagus and the posterior tracheal wall, extending into the mediastinum along the upper thoracic spine at $T_1-T_2$. We have experienced a rare case of occult papillary carcinoma which invaded the trachea, esophagus and fascia of thoracic spine. Treatment was initiated with radioactive iodine and external bean therapy.

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False-positive I-131 Scan by Contaminated Muffler in a Patient with Thyroid Carcinoma (갑상선암 환자에서 방사성 옥소로 오염된 목도리에 의한 위양성 소견)

  • Seo, Han-Kyung;Kim, Min-Woo;Jeong, Hwan-Jeong;Sohn, Myung-Hee
    • Nuclear Medicine and Molecular Imaging
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    • v.40 no.1
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    • pp.51-52
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    • 2006
  • A 39-year-old female patient who had undergone a total thyroidectomy for a papillary thyroid carcinoma underwent a whole body scan with I-131. The I-131 scan was performed 72 hours after administering 185 MBq (5 mCi) of an I-131 solution. The anterior image of the head, neck, and upper chest showed multiple areas of increased uptake in the mediastinal area considering of functional metastasis. However, radioactivity was not evident in the image taken after removing her clothes and muffler. The image obtained after placing the muffler on the pallet showed that the radioactivity was still present. It is well known that artifacts on an I-131 scan can be produced by styling hair sputum, drooling during sleep, chewing gum, and paper or a cloth handkerchief that is contaminated with the radioactive iodine from either perspiration or saliva. This activity might be mistaken for a functional metastasis. Therefore, it is essential that an image be obtained after removing the patient's clothes. In this study, artifacts due to a contaminated muffler on the I-131 scan were found. These mimicked a functional metastasis of the mediastinal area in a patient with a papillary thyroid carcinoma.

Medical Therapeutic Effect of Hyperthyroidism - Comparison of antithyroid therapy and $^{131}I$ Therapy - (갑상선기능항진증(甲狀腺機能亢進症)의 내과적(內科的) 치료효과(治療效果) - 방사성동위원소(放射性同位元素) ($^{131}I$)치료(治療)와 항갑상선제(抗甲狀腺劑) 치료(治療)의 비교검토(比較檢討) -)

  • Lee, Kyu-Bo
    • The Korean Journal of Nuclear Medicine
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    • v.14 no.2
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    • pp.35-40
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    • 1980
  • In order to compare the therapeutic effect as well as side effects between antithyroid therapy and radioiodine therapy in hyperthyroidism, the author evaluated 111 cases of hyperthyroidism which were composed of 57 patients with antithyroid treatment, 23 patients with combined treatment comprising of antithyroid and radioactive iodine ($^{131}I$) and 31 patients with treatment of $^{131}I$ alone. The $^{131}I$ treatment was limited to older age, above 20 years of age, and not employed in patients with pregnancy and lactation. The patients treated with antithyroid belonged to relatively younger age, and also milder in symptoms and thyroid function tests. The remission rate of antithyroid therapy group was 97.8% within 16 months. Among them the early remission rate occured within 4 months was found to be 21.7%. The combined therapy group, having prescribed more severe cases, showed the remission rate to be 75% within 16 months. The remission rate of $^{131}I$ therapy group revealed 90.9% within 16 months. Among them the early remission rate taking place within 4 months disclosed 16.7%. The side effects of antithyroid drug, propylthiouracil, were noted as follows: itching (2.7%) skin rashes (1.3%), and adverse enlargement of goiter (10.7%). The side effects $^{131}I$ therapy were transient hypothyroidism(3.9%) permanent hypothyroidism (7.8%) and itching (2.0%).

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A Case of Mixed Papillary Thyroid Tumor and Squamous-Cell Carcinoma (갑상샘 유두암과 혼재하여 발견된 편평세포암 1예)

  • Kim, Ho-Su;Jung, Tae-Sik;Jung, Jung-Hwa;Kim, Soo-Kyoung;Lee, Sang-Min;Chung, Soon-Il;Hahm, Jong-Ryeal
    • Journal of Yeungnam Medical Science
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    • v.28 no.2
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    • pp.206-210
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    • 2011
  • The occurrence of a mixed tumor containing papillary thyroid carcinoma (PTC) and primary squamous-cell carcinoma (SCC) is rare because there is no squamous epithelium in the thyroid gland. Reported herein is a 30-year-old female with mixed PTC and primary sec of the thyroid presented as thyroid incidentaloma. Fine-needle aspiration biopsy of the thyroid nodule revealed the presence of malignant thyroid cells. The histopathological examination following total thyroidectomy yielded two mixed, morphologically distinct histotypes that included PTC and sec. After total thyroidectomy, the patient underwent radioactive iodine therapy. No recurrence or metastasis occurred during the 20-month follow-up period after the operation.

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The Effects of Iodocasin, Tapazole, and Diethylstilbestrol in the Thyroidal Activities of Chicken (Iodocasein, Tapazole 및 Diethylstilbestrol이 닭의 갑상선기능(甲狀腺機能)에 미치는 영향(影響))

  • Sung, Jai Ki;Yoon, Suk Bong;Kwun, Jong Kuk;Chung, Yung Chai
    • Korean Journal of Veterinary Research
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    • v.8 no.2
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    • pp.54-58
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    • 1968
  • The effects of iodocasein, tapazole, and diethylstilbestrol in the thyroidal activity of chicken were tested. Iodocasein and tapazole were mixed with basal ration at the levels of 0.17 and 0.01 per cent respectively and were fed to one-weeks-old chicken for two months. Six milligrams of diethylstilbestrol were implanted in the subcutaneous tissue. Subsequently 10 uci of radioactive iodine $I^{131}$ were injected intramuscularly into each of the chicken to measure the thyroidal activities of the chicken one month after the treatment was started. The results obtained were as follows: 1) The thyroidal uptake of $I^{131}$ was not observed in the iodocasein group 2) The highest thyroidal uptake rates of I were shown twelve hours after the injection in the all groups except the iodocasein group. 3) The higher thyroidal uptake rates of I were observed in the female chicken than in the male chicken(P<0.01) of the control and the tapazole groups. However, the significant difference between the two sexes was not found in the diethylstilbestrol group. 4) Tapazole at the level of 0.01 per cent of the basal ration of the chicken increased the thyroidal activity slightly.

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Radiological Accident and Acute Radiation Syndrome (방사선 사고와 급성 방사선 증후군)

  • Roh, Hyung-Keun
    • Journal of The Korean Society of Clinical Toxicology
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    • v.9 no.2
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    • pp.39-48
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    • 2011
  • In mass casualty situation due to radiological accidents, it is important to start aggressive management with rapid triage decisions. External contamination needs immediate decontamination and internal contamination should be treated with special expertise and equipment to prevent the rapid uptake of radionuclides by target organs. Acute radiation syndrome shows a sequence of events that varies with the severity of the exposure. More severe exposures generally lead to more rapid onset of symptoms and severe clinical findings. After the massive exposure, various systems of the body reflect their severe damages that can lead to death within hours or up to several months. The disease progression has classically been divided into four stages: prodromal, latent, manifest illness, and recovery or death. Three characteristic clusters of symptoms including the hematopoietic syndrome, the gastrointestinal syndrome and the cerebrovascular syndrome are all associated with the acute radiation syndrome. The standard medical management of the patients with a potentially survivable radiation exposure includes good medical, surgical and supportive measures. Specific treatment with cytokines and bone marrow transplantation should be considered. The management of internal contamination is much the same as the treatment of poisoning. The standard decontamination should be applied to reduce uptake, and the chelating agents can be administered to enhance the clearance of radioisotopes. Radioactive iodine ($^{131}I$) as one of the nuclear fission products can increase the incidence of thyroid cancer in children. Potential benefit of potassium iodide prophylaxis is greater especially in neonates, infants and small children.

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Direct radio-iodination of folic acid for targeting folate receptor-positive tumors

  • Huynh, Phuong Tu;Lee, Woonghee;Ha, Yeong Su;Yoo, Jeongsoo
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.4 no.1
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    • pp.3-10
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    • 2018
  • The folate receptor (FR) is a promising cell membrane-associated target for nuclear imaging of various cancers (via imaging $FR-{\alpha}$) and potentially also inflammatory diseases (via imaging $FR-{\beta}$), through the use of folic acid-based radioconjugates. However, there have been several drawbacks of previously reported radioconjugates, such as a short half-life of the radiolabel ($^{68}Ga\;t_{1/2}$ 68 min), a complex and time-consuming multistep radiosynthesis, and a high renal uptake of radiolabeled folate derivatives. The goal of this study was to develop an imaging probe by directly labeling folate with radioactive iodine without using an extra prosthetic group. The radiolabeling of folate was optimized using various labeling conditions and the labeled tracers were isolated by high-performance liquid chromatography. The in vitro stability of labeled folate was checked in phosphate-buffered saline and serum. The tumor-targeting efficacy of the probe was also evaluated by biodistribution studies using a murine 4T1 tumor model.

The Clinical Study on the Effects of $Tapazole^{(R)}\;upon\;^{131}I$ Uptake in Hyperthyroidism (갑상선(甲狀腺) 기능항진증(機能亢進症)에서 $Tapazole^{(R)}$$^{131}I$섭취율(攝取率)에 미치는 영향(影響)에 관(關)한 임상적(臨床的) 고찰(考察))

  • Ro, Heung-Kyu;Lee, Jung-Sang;Koh, Chang-Soon;Lee, Mun-Ho
    • The Korean Journal of Nuclear Medicine
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    • v.3 no.2
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    • pp.17-22
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    • 1969
  • The differences in the change of the uptake rate of radioactive iodine ($^{131}I$) in the thyroid gland after $Tapazole^{(R)}$ administration before $^{131}I$ treatment were analysed in 137 patients who were diagnosed as diffuse toxic goiter in the Radioisotope Clinic and Laboratory, Seoul National University Hospital since Jan. 1967 to July, 1969. The uptake rate of the therapeutic dose of $^{131}I$ was changed diffusely compared with that of the trace dose in the patients who had no $Tapazole^{(R)}$ administration before $^{131}I$ treatment. In those patients who had $Tapazole^{(R)}$ more than 20 mg/day for more than one week before $^{131}I$ treatment, the uptake rate was decreased significantly. When the patients discontinued the administration of $Tapazole^{(R)}$ 7 days prior to $^{131}I$ treatment, the uptake rate was increased in all cases.

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