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Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging
Author(s) -
Swidan M. M.,
Sakr T. M.,
Motaleb M. A.,
ElBary A. Abd,
ElKolaly M. T.
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3223
Subject(s) - acebutolol , chemistry , in vivo , myocardial perfusion imaging , perfusion , radiochemistry , pharmacology , medicine , microbiology and biotechnology , blood pressure , biology
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.