1. Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging.
- Author
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Swidan MM, Sakr TM, Motaleb MA, El-Bary AA, and El-Kolaly MT
- Subjects
- Acebutolol chemical synthesis, Animals, Iodine Radioisotopes chemistry, Iodine Radioisotopes pharmacokinetics, Male, Mice, Radiopharmaceuticals chemical synthesis, Tissue Distribution, Acebutolol pharmacokinetics, Myocardial Perfusion Imaging methods, Radiopharmaceuticals pharmacokinetics
- Abstract
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.)
- Published
- 2014
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