1.A novel strategy for synthesis of 5-iodo ((125/131)I)-1, 2, 3-triazoles via click chemistry.
Cheng WANG ; Jilin YIN ; Wei ZHOU ; Lan ZHANG ; Zheng ZHOU
Journal of Southern Medical University 2013;33(6):779-784
We report a facile and effective method for radioiodine-labeled radiopharmaceuticals via copper (I)-catalyzed click chemistry route. In the novel radioiodination method, 5-iodo ((125/131)I)-1, 2, 3-triazoles were synthesized after a 24-h click reaction in organic solvent with a radiochemical yield of 13%. However, in the aqueous phase, the radiochemical yield of the conjugation radioiodine to RGD via click chemistry was 0. This suggested an exchange between hydrogen ion and iodine ion in aqueous phase so that no enough radioiodine was left to conjugate with RGD. We propose different mechanisms of Cu (I)-catalyzed cycloaddition of organic azides and 1-iodo-alkynes in organic phase and aqueous phase.
Click Chemistry
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Iodine Radioisotopes
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Radiopharmaceuticals
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chemical synthesis
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Triazoles
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chemical synthesis
2.Radioactivity of phosphorus implanted TiNi alloy.
Xingke ZHAO ; Wei CAI ; Liancheng ZHAO
Journal of Biomedical Engineering 2003;20(3):412-414
Exposed to neutron flow, the phosphorus implanted TiNi alloy gets radioactive. This radioactive material is used in vascular stent for prevention and cure of restenosis. Phosphorus implantation is carried out in a plasma immerged ion implantation system, and the dose of phosphorus implantation is in the range of 2-10 x 10(17) cm-2. After ion implantation, the alloy is exposed to the slow neutron flow in a nuclear reactor, the dose of the slow neutron is 1.39-5.88 x 10(19) n/cm2. The radioactivity of the TiNi alloy was measured by liquid scintillation spectrometry and radio-chromic-film dosimetry. The result shows that whether the phosphorus is implanted or not, the TiNi alloy comes to be radioactive after exposure to neutron flow. Just after neutron irradiation, the radiation dose of phosphorus implanted TiNi alloy is about one hundred times higher than that of un-phosphorus implanted TiNi alloy. The radiation difference between phosphorus and un-phosphorus implanted alloy decreases as time elapses. Within three months after neutron irradiation, the average half-decay period of phosphorus implanted TiNi alloy is about 62 days. The radiation ray penetration of phosphorus implanted TiNi alloy is deeper than that of pure 32P; this is of benefit to making radiation uniformity between stent struts and reducing radiation grads beyond the edge of stent.
Alloys
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chemistry
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Blood Vessel Prosthesis
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Nickel
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chemistry
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Phosphorus Radioisotopes
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chemistry
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Radiation Dosage
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Titanium
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chemistry
3.Labeling of CDTPA-dianhydride-coupled CD45 monoclonal antibody with yttrium-90.
Yun-bi FU ; Gui-ping LI ; Fan-yi MENG
Journal of Southern Medical University 2006;26(8):1230-1232
OBJECTIVETo explore the methods for labeling CDTPA-coupled CD45 monoclonal antibody (mAb) with yttrium-90 ((90)Y) for potential acute myeloid therapy.
METHODSCD45 mAb was labeled with (90)Y by CDTPA and the labeling rate, radiochemical purity, final specific activity, and immunological activity of the mAb were detected.
RESULTSWith the optimal molar ratio of CDTPA/Ab at 20:1, the labeling rate was 95%, radiochemical purity 99.8%, and final specific activity 1.9 mCi/mg. This conjugate was stable in vitro with comparable immunological activity in comparison with unlabeled CD45 mAb.
CONCLUSION(90)Y-CDTPA-CD45 mAb possesses good properties as an ideal targetting therapeutic agent for acute leukemia.
Anhydrides ; chemistry ; Antibodies, Monoclonal ; chemistry ; immunology ; Humans ; Immunoconjugates ; chemistry ; immunology ; Isotope Labeling ; methods ; Leukocyte Common Antigens ; immunology ; Pentetic Acid ; chemistry ; Radiopharmaceuticals ; chemical synthesis ; chemistry ; immunology ; Yttrium Radioisotopes ; chemistry
4.Automated microfluidic chip system for radiosynthesis of PET imaging probes.
Ming LEI ; Jian-Zhang PAN ; Guang-Ming XU ; Pei-Zhen DU ; Mei TIAN ; Hong ZHANG
Journal of Zhejiang University. Science. B 2019;20(11):865-867
Positron emission tomography (PET) is a powerful non-invasive molecular imaging technique for the early detection, characterization, and "real-time" monitoring of disease, and for investigating the efficacy of drugs (Phelps, 2000; Ametamey et al., 2008). The development of molecular probes bearing short-lived positron-emitting radionuclides, such as 18F (half-life 110 min) or 11C (half-life 20 min), is crucial for PET imaging to collect in vivo metabolic information in a time-efficient manner (Deng et al., 2019). In this regard, one of the main challenges is rapid synthesis of radiolabeled probes by introducing the radionuclides into pharmaceuticals as soon as possible before injection for a PET scan. Although many potential PET probes have been discovered, only a handful can satisfy the demand for a highly efficient synthesis procedure that achieves radiolabeling and delivery for imaging within 1-2 radioisotope half-lives. Only a few probes, such as 2-deoxy-2-[18F]fluoro-D-glucose (18F-FDG) and [18F]fluorodopa, are routinely produced on a commercial scale for daily clinical diagnosis (Grayson et al., 2018; Carollo et al., 2019).
Lab-On-A-Chip Devices
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Positron-Emission Tomography/methods*
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Radioisotopes/chemistry*
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Radiopharmaceuticals/chemical synthesis*
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Solid Phase Extraction
5.Nano-size uni-lamellar lipodisq improved in situ auto-phosphorylation analysis of E. coli tyrosine kinase using (19)F nuclear magnetic resonance.
Dong LI ; Juan LI ; Yonglong ZHUANG ; Longhua ZHANG ; Ying XIONG ; Pan SHI ; Changlin TIAN
Protein & Cell 2015;6(3):229-233
Escherichia coli
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enzymology
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Fluorine Radioisotopes
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analysis
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Lipid Bilayers
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chemistry
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Magnetic Resonance Spectroscopy
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Maleates
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chemistry
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Nanoparticles
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chemistry
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Phosphorylation
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Polystyrenes
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chemistry
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Protein Conformation
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Protein-Tyrosine Kinases
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chemistry
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metabolism
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Tyrosine
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metabolism
6.Is It Safe to Eat Fish?.
Yu Kyeong KIM ; Keon Wook KANG ; Seung Kwon HONG ; Kyung Hee CHO ; Ho Sin CHOI
Journal of Korean Medical Science 2013;28(12):1701-1702
No abstract available.
Animals
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Cesium Radioisotopes/analysis/chemistry
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*Environmental Exposure
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Half-Life
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Humans
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Perciformes/metabolism
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Seafood/*analysis
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Water Pollutants, Radioactive/*analysis/chemistry
7.Shielding property of different prosthetic materials to shield radiation of (125)I seed.
Yang BAI ; Yan-yi WANG ; Lei ZHANG ; Rong-fa BU
Chinese Journal of Stomatology 2011;46(8):502-504
OBJECTIVETo investigation the shielding property to (125)I of several different prosthetic materials used in clinical when prostheses are used as carriers of (125)I seed in tumor treatment.
METHODS(125)I seeds were taken as the radiation sources to establish a model in vitro and the radiation doses were measured by thermoluminescent dosemeters (TLD). The shielding property of titanium plate, cochrome plate, and poly methyl methacrylate (PMMA) plate were detected, calculated and compared with that of plumbum plate in the control group.
RESULTSThe radiation doses of the radiation source at 10 mm distance through the following materials were measured, and the results are 2.805 mGy (0.09 mm thick titanium plate), 1.082 mGy (0.48 thick titanium plate), 0.390 mGy (0.41 mm thick cochrome plate), and 0.261 mGy (0.67 mm's cochrome plate), and 2.885 mGy (1.685 mm thick PMMA plate).
CONCLUSIONSThe shield property of cochrome is optimal. The poly methyl methacrylate behaves to some extend as a shield to the (125)I seed which can shield the radiation as the effects of plumbum when adopted together with the 0.557 mm's (or more) titanium plate.
Brachytherapy ; Chromium ; chemistry ; Cobalt ; chemistry ; Dental Materials ; Dental Prosthesis ; Iodine Radioisotopes ; Polymethyl Methacrylate ; chemistry ; Protective Devices ; Radiation Dosage ; Radiation Protection ; instrumentation ; Thermoluminescent Dosimetry ; Titanium ; chemistry
8.Estimates of Radiation Doses and Cancer Risk from Food Intake in Korea.
Eun Kyeong MOON ; Wi Ho HA ; Songwon SEO ; Young Woo JIN ; Kyu Hwan JEONG ; Hae Jung YOON ; Hyoung Soo KIM ; Myung Sil HWANG ; Hoon CHOI ; Won Jin LEE
Journal of Korean Medical Science 2016;31(1):9-12
The aim of this study was to estimate internal radiation doses and lifetime cancer risk from food ingestion. Radiation doses from food intake were calculated using the Korea National Health and Nutrition Examination Survey and the measured radioactivity of 134Cs, 137Cs, and 131I from the Ministry of Food and Drug Safety in Korea. Total number of measured data was 8,496 (3,643 for agricultural products, 644 for livestock products, 43 for milk products, 3,193 for marine products, and 973 for processed food). Cancer risk was calculated by multiplying the estimated committed effective dose and the detriment adjusted nominal risk coefficients recommended by the International Commission on Radiation Protection. The lifetime committed effective doses from the daily diet are ranged 2.957-3.710 mSv. Excess lifetime cancer risks are 14.4-18.1, 0.4-0.5, and 1.8-2.3 per 100,000 for all solid cancers combined, thyroid cancer, and leukemia, respectively.
Adolescent
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Adult
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Cesium Radioisotopes/chemistry
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Child
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Child, Preschool
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*Eating
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Food Contamination, Radioactive/*analysis
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Humans
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Infant
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Infant, Newborn
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Iodine Radioisotopes/chemistry
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Neoplasms, Radiation-Induced/*etiology
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Nutrition Surveys
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Radiation Dosage
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Republic of Korea
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Young Adult
9.Study on the preserving techniques of squeezed juice of fresh ginger and Glutinous rehannia.
Hua YANG ; Jin-da HAO ; Ji-ping LI ; Hong YI ; Hua MA
China Journal of Chinese Materia Medica 2003;28(12):1145-1148
OBJECTIVETo study the preserve techniques of squeezed juice of Chinese medicinal materials.
METHODThe techniques of refrigeration, rapid freezing, 60Cogamma-ray sterilization, freeze-drying and spray-drying were used for preservation of squeezed juice of Ginger and Glutinous Rehannia. Different results were compared.
RESULTThe period of preservation was half or one year.
CONCLUSIONThe rapid freezing, freeze-drying and spray-drying are suitable for preservation of squeezed juice of Chinese medicinal materials.
Cobalt Radioisotopes ; Cryopreservation ; Drug Storage ; methods ; Freeze Drying ; methods ; Freezing ; Ginger ; chemistry ; Oils, Volatile ; analysis ; Polysaccharides ; analysis ; Refrigeration ; Rehmannia ; chemistry ; Sterilization
10.Pharmacokinetic parameter and residua of 63Ni-NiCl2 in rat.
Zhan LI ; Hao WANG ; Wang-Suo WU
Acta Pharmaceutica Sinica 2008;43(2):224-226
Absorption distribution and excretion of 63Ni-NiCl2, administered orally to rats were studied by using liquid scintillation counting method. It was observed that the concentration-time curves in blood fitted the two compartment model of pharmacokinetics, Ka=6.18 h(-1), T(1/2)alpha =0.79 h, T(1/2)beta=40.68 h, CL =0.42 mL kg(-1) h(-1), Tmax =0.53 h, Cmax=24,987.75 min(-1) mL(-1), and Vd=0.016 L kg(-1). After rats were treated by 63Ni-NiCl2 for 15 days, in 22 tissues tested, the contents of 63Ni-NiCl2 in hair, hypothalamus, hypophysis, pancreas, small and large intestines were higher, and the residua of 63Ni-NiCl2 was not discovered in liver, kidney and heart. Radioactivity eliminated was 83.27% by urine and feces, 54.86% by urine, 28.41% by feces.
Administration, Oral
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Animals
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Area Under Curve
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Feces
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chemistry
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Female
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Hair
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metabolism
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Nickel
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pharmacokinetics
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urine
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Radioisotopes
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pharmacokinetics
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urine
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Random Allocation
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Rats
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Rats, Sprague-Dawley
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Tissue Distribution