[Radiochemistry of aqueous, oxygen-containing solutions of 5-bromouracil (II). Reaction of the OH-radical with bromouracil].
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Records of pollution by plutonium and americium 241 of skin wounds and burns in the personnel of the Mayak plant in 1948-1992 are analyzed. Traumas occurred in 286 (7.2%) workers, mechanical injuries were 84.1% of these. A high incidence of wound contamination was recorded in the workers engaged in mechanical processing of plutonium. Altogether 34.1% of injuries had alpha-radiators in residual amounts after debridement, though their levels did not surpass the minimal levels of radionuclide detection.
Bifunctional chelating agents based on benzyl-EDTA bind 111In stably under physiological conditions. Available evidence indicates that the indium is cleared from the body in its original chelated form. Initial studies of a series of antibody-chelate conjugates joined by different molecular linkers show that the 111In biodistribution is strongly dependent on the nature of the linker. Linkers containing thiourea, thioether, peptide, ester, and disulfide groups were compared in healthy BALB/c mice. The disulfide linker led to particularly rapid clearance of 111In from the liver, and from the whole body. Results did not appear to be as favorable as those currently obtainable with reversible radiolabelling techniques, in which the 111In chelate is bound non-covalently to the antibody and a competing hapten is used to displace it when desired. However, the concept of a metabolically cleavable linker is sound. Further exploration is needed to produce a conjugate with the desired properties.
Metaiodobenzylguanidine (MIBG) is actively concentrated in adrenergic neuroendocrine tissues and tumors by an active, energy- and sodium-dependent, high-affinity, saturable mechanism. This has proved successful, when labeled with 131-I or 123-I, in scintigraphically depicting pheochromocytomas and neuroblastomas. For imaging purposes 123-I has multiple advantages over 131-I; the gamma ray energy is ideal for modern instruments, the decay by electron capture limits the particulate emissions, and the short half-life reduces the radiation burden. It is thus possible to use doses of 123-I-MIBG 20 times as large as doses of 131-I-MIBG with equivalent absorbed radiation doses. Disadvantages of 123-I include the cost and difficulties in the regular delivery of this short-lived radionuclide. For most imaging purposes 123-I-MIBG is the optimal agent if logistical problems in its supply can be overcome.
A new derivative of octreotide SDZ 219-387 [PnAO-(D)Phe(1)-octreotide] was synthesized, which binds specifically and with high affinity to somatostatin receptors in vitro (pKi = 9.79 +/- 0.16). This new somatostatin analogue chelates technetium-99m under mild labelling conditions in good yields. The resulting [99mTc]SDZ 219-387 was stable up to 6 h after labelling and could be isolated in a pure radiochemical and chemical form by high-performance liquid chromatographic purification. The intravenous administration of purified [99mTc]SDZ 219-387 revealed that the radioligand was rapidly cleared from circulation, and tumour uptake of 0.38% ID/g was observed at 1.5 h post injection. [99mTc]SDZ 219-387 specifically interacted with somatostatin binding sites on the tumour. However, the radioligand is highly lipophilic and excreted mainly through the hepatobiliary system. As a consequence, [99mTc]SDZ 219-387 exhibits increased background activity and therefore is not appropriate for the in vivo visualization of somatostatin receptor-positive tumours and/or their metastases in the abdomen.
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The synthesis, radiochemical analysis and biological characteristics of some 1,8-diamine-3,6-dithiaoctane derivatives labelled with Tc-99m are reported. Analysis by HPLC shows that most of the 99mTc-chelates are multicomponent. Furthermore, almost all 99mTc-complexes isolated by HPLC are lipophilic and stable in vitro. The biodistributions of the most lipophilic of these complexes were evaluated in mice. The N-morpholinylethyl and N,N'-bisalicylyl derivatives of 1,8-diamine-3,6-dithiaoctane yielded 99mTc-complexes which exhibit considerable uptake and retention in organs of interest, such as the heart and the brain.
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This paper summarizes the methods currently applied by the National Institute of Standards and Technology (NIST) for the preparation and verification of environmental and radiobioaasay performance evaluation materials for the traceability testing of low-level radioactivity measurements. The evaluation of measurement quality of the all participants indicated that over 90% of the intercomparison results complied with ANSI N42.22 and/or HPS N13.30 standards. Overall, the differences from the NIST values observed for all test nuclides and matrices are less than -7%, with a typical measurement precision better than 10% (1 s). The dependency of measurement quality on the test radionuclides, sample matrices, and radiochemical methods is identified by statistical analyses.
At the Rossendorf PET Centre the PET cyclotron and the radiochemical laboratories are 500 m away from each other. The distance is bridged by a radionuclide transport system (RATS) whose details such as layout, technical parameters, control system and radiation protection are described along with our experience in long-distance transport of radionuclides.
105Rhodium(III) complexes with three different acyclic tetrathioether ligands containing pendant carboxylic acid groups have been synthesized and characterized. The complexes were evaluated for stability under physiological conditions and the most promising complexes were evaluated in vivo in normal mice. The primary route of clearance for these complexes was the renal/urinary system, consistent with the presence of pendant carboxylate groups. The results indicate that the cis-[Rh(III)Cl2(2,5,8,11-tetrathiadodecane-1,12-dicarboxylic acid)]+ complex shows the most promising in vivo characteristics on which to base a potential therapeutic radiopharmaceutical.