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  • Author or Editor: G. El-Shaboury x
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Abstract  

Radioiodinated 4-[*I]iodoantipyrine labeled with radioiodine (i.e., 123I or 125I or 131I) has been used for modeling radiation damage on cell nuclei of tumor cells where the characteristic high linear energy transfer (high-LET) of the Auger electron could be demonstrated. Also, the compound is currently used for the measurement of regional cerebral blood flow (rCBF) in autoradiography. 4-[131I]iodoantipyrine was synthesized by two methods via a nucleophilic isotopic exchange reaction between 131I as iodide ion [131I] and inactive 4-[127I]iodoantipyrine: either in absolute ethyl alcohol catalyzed by ammonium acetate or in dry state molten ammonium acetate (m.p. 114 °C) as an isotopic exchange medium without carrier addition. The first one is called wet method: where a solution of 4-iodoantipyrine and ammonium acetate in absolute ethyl alcohol and lyophilized Na131I was heated briefly up to boiling (80 to 90 °C) for 30 minutes under reflux. The second one is called dry state-molten method: where the alcoholic solution containing 4-iodoantipyrine and ammonium acetate and the lyophilized Na131I were heated briefly in a nitrogen stream to dryness at 120 to 125 °C for 5 minutes or melted by gradual heating at 150 to 160 °C for 5 minutes. A radiochemical yield ranged between 90%–95% in each method has been obtained for 4-[131I]iodoantipyrine. In both methods, the reaction proceeds properly without carrier addition by an addition – elimination mechanism. The physico-chemical parameters affecting the radiochemical yield of the isotopic exchange reaction [i.e., reaction time, temperature, exchange medium, concentration of the reactants, carrier (KI) addition and pH] were investigated. Chromatographic analysis i.e., TLC and HPLC were used to determine the radiochemical yield as well as the purity of the final product, which was as pure as 99.9%.

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Abstract  

The exchange of Rose-Bengal in the mono-sodium salt with elementary131I in an organic medium allows for the preparation of a labelled product substantially higher in radiochemical purity than that produced by other methods. Purification of the starting material before the labelling process has been done by adsorption chromatography. Under the conditions described a radiochemical yield more than 97% can be obtained within 30–60 minutes. The product was stable during sterilization and storage for 10 days and was found to be free of131I.

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Abstract  

The present investigation deals with a study of the isotope exchange reaction of iodine between sodium iodide [Na131I] and [4-127I]iodoantipyrine in organic medium, using different iodinating radioiodine reagents of different carrier-iodine concentration. A maximum saturation yield over 90% of pure [4-131I]iodoantipyrine has been obtained by performing the isotope exchange reaction in ethanol at 80°C in 30 min. The same yield has been obtained using the same concentrations by performing the reaction at room temperature (17–20°C) for 3 h. Also the rate of the isotope exchange reaction was found to be carrier-iodine dependent as well as time and temperature dependent. According to these results and reaction conditions, a kit form method was elaborated for the synthesis of [4-131I]iodoantipyrine as well as [4-123I]iodoantipyrine.

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