Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging

Autor:	M. A. Motaleb, Tamer M. Sakr, M. T. El-Kolaly, A. Abd El-Bary, Mohamed M. Swidan
Rok vydání:	2014
Předmět:	medicine.diagnostic_test Chemistry Organic Chemistry Pharmacology Myocardial imaging Highly selective Biochemistry In vitro Acebutolol Analytical Chemistry Myocardial perfusion imaging In vivo Drug Discovery medicine Distribution (pharmacology) Radiology Nuclear Medicine and imaging Receptor Spectroscopy medicine.drug
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals. 57:593-599
ISSN:	0362-4803
DOI:	10.1002/jlcr.3223
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::fe76b912c2b5cf43394219b540629a29 https://doi.org/10.1002/jlcr.3223 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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