RESUMO
Excitation functions were measured by the activation method using stacked-foil technique for the natSr(p,xn)88,87m,g,86m,gY reactions up to 18â¯MeV. The experimental results were compared with the theoretical data from EMPIRE-3.2 code and TENDL. Integral yields of 88,87m,g,86m,gY were estimated based on the measured cross sections. The optimum energy range for the production of the important isotope 88Y is Epâ¯=â¯16â11â¯MeV, 88Y yield amounts to about 3 MBq/µAh.
RESUMO
The rapid synthesis of two radiofluoronicotinamide derivatives, namely, [18F]MEL050 and [18F]MEL-2F has been simply performed starting from commercial materials. [18F]MEL-2F is a new, potential analogue PET-probe for melanoma imaging. [18F]MEL050 is already an excellent PET imaging probe for early specific diagnosis. The synthesis involves coupling step to obtain the precursor followed by radiofluorination. During the synthesis of the precursors different coupling reagents, such as HBTU, TFFH, HOBT, COMU and PyCIU have been applied. PyClU was found the best to reduce the coupling period to < 1h. The labeled compounds were isolated and purified by HPLC. In the in-vitro study three kinds of cells, namely, Melur (melanin free), KB-3 carcinoma cell line (non-melanoma) and B16-F10 melanoma cell line were used to evaluate the uptake of the radiotracers.
Assuntos
Radioisótopos de Flúor/química , Melanoma Experimental/diagnóstico por imagem , Niacinamida/síntese química , Compostos Radiofarmacêuticos/química , Animais , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão , Radioisótopos de Flúor/farmacocinética , Indicadores e Reagentes/química , Espectrometria de Massas , Melanoma Experimental/metabolismo , Melanoma Experimental/patologia , Camundongos , Niacinamida/química , Niacinamida/farmacocinética , Espectroscopia de Prótons por Ressonância Magnética , Compostos Radiofarmacêuticos/farmacocinéticaRESUMO
Radioiodinated MIP-1145, which specifically targets melanin, is an ideal candidate for targeted therapy of melanoma. An analogue of MIP-1145 lacking the iodo-substituent (desiodo-MIP-1145) was synthesized as a labeling precursor in three simple steps. The radioiodination of desiodo-MIP-1145 by iodine-125 was carried out via an electrophilic substitution reaction. An optimization study for the iodination reaction was carried out. The labeled compound was isolated and purified by means of electrophoresis and HPLC. The maximum radiochemical yield, 76%, was obtained with radiochemical purity greater than 99%. The log P value for [(125) I]MIP-1145 was measured as 4.5.
Assuntos
Benzamidas/química , Benzamidas/síntese química , Radioisótopos do Iodo , Melanoma/diagnóstico por imagem , Imagem Molecular/métodos , Técnicas de Química Sintética , Marcação por Isótopo , RadioquímicaRESUMO
Proton induced nuclear reactions were measured with stacked-foil technique on natural zirconium targets up to 16.7MeV. Excitation functions were measured for the production of (90,92m,95m,95g,96)Nb and (88)Y. Cumulative cross-section, thick target yields and activation functions were deduced and compared with the available experimental data, as well as with the nuclear models codes; ALICE-IPPE, EMPIRE and TALYS. The integral yields for thick targets were deduced from the measured excitation function of the produced radionuclides.
