Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging. (5th September 2014)

• Record Type: Journal Article
• Authors: Swidan, M. M.; Sakr, T. M.; Motaleb, M. A.; El‐Bary, A. Abd; El‐Kolaly, M. T.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 57:Number 10(2014)
• Page Start: 593
• Page End: 599
• Publication Date: 2014-09-05
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3223
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>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 <italic>in vitro</italic> stability up to 72 h. The <italic>in vivo</italic> 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. <italic>In vivo</italic> 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.</p> </abstract>