Journal
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Volume 57, Issue 10, Pages 593-599Publisher
WILEY
DOI: 10.1002/jlcr.3223
Keywords
myocardial perfusion imaging; radioiodination; acebutolol; chloramin-T
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Acebutolol was successfully labeled with I-125 via direct electrophilic substitution reaction. Radioiodinated acebutolol was prepared with a maximum radiochemical yield of 96.5 +/- 0.3% and in vitro stability up to 72h. The in vivo biological distribution of radioiodinated acebutolol showed high heart uptake of 37.8 +/- 0.14% injected activity/g organ with low lungs and liver uptakes at 5min post-injection. In vivo receptor blocking study was carried out in mice to evaluate its selectivity to heart. Radioiodinated acebutolol showed fast heart accumulation with high heart/liver ratio, which provides the ability for fast myocardial imaging with significant decrease in the radiation hazards risk on patients. So, radioiodinated acebutolol could be displayed as a radiotracer drug of choice in case of emergency patients for myocardial perfusion imaging.
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