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 ; Iodine Radioisotopes ; Radiopharmaceuticals ; chemical synthesis ; Triazoles ; chemical synthesis

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 ; chemistry ; Blood Vessel Prosthesis ; Nickel ; chemistry ; Phosphorus Radioisotopes ; chemistry ; Radiation Dosage ; Titanium ; chemistry

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

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 ; Positron-Emission Tomography/methods* ; Radioisotopes/chemistry* ; Radiopharmaceuticals/chemical synthesis* ; Solid Phase Extraction

Escherichia coli ; enzymology ; Fluorine Radioisotopes ; analysis ; Lipid Bilayers ; chemistry ; Magnetic Resonance Spectroscopy ; Maleates ; chemistry ; Nanoparticles ; chemistry ; Phosphorylation ; Polystyrenes ; chemistry ; Protein Conformation ; Protein-Tyrosine Kinases ; chemistry ; metabolism ; Tyrosine ; metabolism

No abstract available.
Animals ; Cesium Radioisotopes/analysis/chemistry ; *Environmental Exposure ; Half-Life ; Humans ; Perciformes/metabolism ; Seafood/*analysis ; Water Pollutants, Radioactive/*analysis/chemistry

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 ; Adult ; Cesium Radioisotopes/chemistry ; Child ; Child, Preschool ; *Eating ; Food Contamination, Radioactive/*analysis ; Humans ; Infant ; Infant, Newborn ; Iodine Radioisotopes/chemistry ; Neoplasms, Radiation-Induced/*etiology ; Nutrition Surveys ; Radiation Dosage ; Republic of Korea ; Young Adult

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

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 ; Animals ; Area Under Curve ; Feces ; chemistry ; Female ; Hair ; metabolism ; Nickel ; pharmacokinetics ; urine ; Radioisotopes ; pharmacokinetics ; urine ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tissue Distribution

Prostate cancer is the most common tumor of the urinary system, and its mortality rate is second only to lung cancer. With the specific and high expression on the surface of prostate cancer cells, prostate-specific membrane antigen (PSMA) has been an ideal theranostic target of prostate cancer with great clinical significance and research value. Positron emission tomography/computed tomography (PET/CT), a new modality of molecular imaging combining functional metabolic information and anatomical structure, provides high diagnostic performance for cancer detection. This paper mainly reviewed recent progress of PSMA inhibitors labeled by positron-emitting radionuclides for early diagnosis, preoperative staging, response assessment, restaging and metastasis detection of prostate cancer.
Electrons ; Humans ; Kallikreins ; antagonists & inhibitors ; Male ; Positron Emission Tomography Computed Tomography ; Prostate-Specific Antigen ; antagonists & inhibitors ; Prostatic Neoplasms ; diagnostic imaging ; Radioisotopes ; chemistry