Synthesis of a 125I-radiolabeled penicillin for penicillin-binding proteins studies.

Radioiodination of penicillin X (p-hydroxybenzylpenicillin) with 125INa, using the chloramine-T method, is simple and almost quantitative. The product thus obtained can be used without further purification for the penicillin-binding proteins (PBPs) assay. The chemical structure of 125I-penicillin X is very close to that of penicillin G, and the affinity of the two compounds for the PBPs are very similar. 125I-penicillin X can then advantageously replace [14C]penicillin G in these experiments, as its specific radioactivity is 2000 Ci/mol, in our preparations, instead of about 50 Ci/mol; thus, the experimental procedure is simplified and the autoradiography exposure time is reduced to 12-48 h.