Swidan, MMSakr, TMMotaleb, MAAbd El‐Bary, AEl‐Kolaly, MT2020-02-132020-02-1320141099-1344https://doi.org/10.1002/jlcr.3223https://cutt.ly/HrLqMhlMSA Google ScholarAcebutolol 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.enmyocardial perfusion imagingradioiodinationacebutololchloramin‐TArticlehttps://doi.org/10.1002/jlcr.3223