Abstract
Cefaclor and ampicillin, β-lactam antibiotics capable to penetrate the outer membrane of Grampositive and some Gram-negative bacteria, were labeled with 125I via electrophilic substitution of the hydrogen atom with the iodonium ion I+. The reaction yield strongly depends on pH of the medium, reaching a maximum at pH 7. This may be due to efficient protonation and high performance of the oxidizing agent at this pH value. In alkaline solutions, the labeling yield decreased, because cefaclor and ampicillin are unstable at these pH values. The produced 125I-cefaclor and 125I-ampicillin are stable in vivo, as the thyroid gland uptake does not exceed 1.2%. Labeled cefaclor and ampicillin are efficiently localized in bacterial inflamed muscle. The abscess to muscle ratio for 125I-cefaclor and 125I-ampicillin was found to be 5.1 and 6.8, respectively. The imaging should be carried out at 2 h post injection, because at this time the activity is concentrated in the target site and the background activity has been cleared.
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Published in Russian in Radiokhimiya, 2014, Vol. 56, No. 4, pp. 368–372.
The text was submitted by the authors in English.
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Amin, A.M., Magdy, M. & Abd El-Bary, A. Comparative study of labeling conditions and biodistribution of 125I-cefaclor and 125I-ampicillin for infectious foci imaging. Radiochemistry 56, 433–438 (2014). https://doi.org/10.1134/S1066362214040134
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DOI: https://doi.org/10.1134/S1066362214040134