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EN
Targeting apoptosis is an interesting issue in molecular imaging and various modalities have been presented. However, recent experiences in nuclear pharmacy demonstrated the application of small tracer molecules is more desired. This work was conducted for production of a radiolabeled copper complex, i.e. 61Cu-oxinate as a potential PET tracer for apoptosis imaging in oncology. Cu-61 was prepared by natural zinc target irradiation with 22 MeV protons (150 miA) via the natZn(p, xn)61Cu nuclear reaction with a yield of 3.33 mCi/miAh. In order to obtain the best labeling method, optimization reactions were performed for pH, temperature and concentration followed by solid phase extraction. Biodistribution of the tracer was studied in wild-type and fibrosarcoma bearing mice. Under the optimized conditions, radio-thin-layer chromatography (RTLC) and HPLC showed radiochemical purities of 99.99% and 97% respectively (with a minimum specific activity of 16 Ci/mM). Biodistribution of the tracer in fibrosarcoma bearing mice demonstrated a significant tumor uptake after 3 h. Tumor:blood and tumor:muscle ratios were 2.0 and 6.0 after 3 h, respectively.
EN
Human polyclonal antibody (HIgG) was successively labeled with 111In-indium chloride after residulation with freshly prepared cyclic DTPA-dianhydride. The best results of the conjugation were obtained by the addition of solid DTPA-dianhydride (0.1 0.3 mg) to 100 mi l of the HIgG solution (0.2 0.4 mg/ml) at pH = 6 in phosphate buffer media at 25°C with continuous stirring for 30 min. Radio-thin-layer chromatography showed an overall radiochemical yield of 96 99% at optimized conditions (specific activity = 300 500 MBq/mg, radiochemical purity >98%). The final isotonic 111In-DTPA-HIgG complex was checked by radio-TLC to ensure the formation of only one species followed by filtration through a 0.22 mi filter. Preliminary long-term in vivo studies in turpentine-oil induced inflammation in rat model was performed to determine late complex distribution of the radioimmunoconjugate. The target/skin and target/ blood ratios were 27 and 51 after 24 h, and 23 and 51 after 110 h, showing a high selectivity of the radiopharmaceutical for inflammatory lesions.
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