Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging |
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| Authors: | M. M. Swidan T. M. Sakr M. A. Motaleb A. Abd El‐Bary M. T. El‐Kolaly |
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| Affiliation: | 1. Labeled Compound Department, Hot Labs Center, Atomic Energy Authority, Cairo, Egypt;2. Radioactive Isotopes and Generator Department, Hot Labs Center, Atomic Energy Authority, Cairo, Egypt;3. Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt |
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| Abstract: | Acebutolol was successfully labeled with 125I 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. |
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| Keywords: | myocardial perfusion imaging radioiodination acebutolol chloramin‐T |
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