Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging.

Acebutolol was successfully labeled with (125) I 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 72 h. 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 5 min 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. Copyright © 2014 John Wiley & Sons, Ltd.

Citation

M M Swidan, T M Sakr, M A Motaleb, A Abd El-Bary, M T El-Kolaly. Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging. Journal of labelled compounds & radiopharmaceuticals. 2014 Aug;57(10):593-9

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PMID: 25196119

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