Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation
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Date
2018
Journal Title
Journal ISSN
Volume Title
Type
Article
Publisher
Elsevier Ltd
Series Info
Applied Radiation and Isotopes
137
137
Scientific Journal Rankings
Abstract
Challenges facing cardiovascular imaging necessitate innovation of better radiopharmaceuticals to augment or replace the existing ones. This research assesses the ability and competency of radioiodinated esmolol as a potential cardio selective imaging agent. Radioiodinated esmolol was synthesized with 97.3 � 0.3% radiochemical yield and with high stability up to 48 h at room temperature as well as in rat serum. Molecular modeling study was performed to confirm the binding of iodinated esmolol to ?1-adrenergic receptor. Its biodistribution studies in normal Swiss albino mice showed high heart uptake (38.5 � 0.11%ID/g at 5 min p.i.), heart/liver ratio nearly 3.85:1 and heart/lungs ratio was about 7:1 at 5 min p.i. The evidenced selectivity of the radioiodinated esmolol to ?1-adrenoceptor was confirmed by prior injection of cold esmolol. Gamma camera biodistribution pattern showed that radioiodinated esmolol accumulated selectively in heart. � 2018 Elsevier Ltd
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Keywords
October University for Modern Sciences and Arts, University for Modern Sciences and Arts, MSA University, جامعة أكتوبر للعلوم الحديثة والآداب, Cardiac imaging, Esmolol, Gamma scintigraphy, Molecular modeling, Radioiodination, Molecular modeling, Nuclear medicine, Adrenergic receptors, Cardiac imaging, Esmolol, Gamma scintigraphies, Molecular modeling studies, Myocardial perfusion imaging, Radiochemical yield, Radioiodination, Heart, beta 1 adrenergic receptor, cyanopindolol, di iodinated esmolol, esmolol, mono iodinated esmolol, tracer, unclassified drug, beta 1 adrenergic receptor, esmolol, Iodine-131, propanolamine derivative, radioactive iodine, radiopharmaceutical agent, animal experiment, Article, cardioselectivity, computer model, drug receptor binding, gamma scintigraphy, in vitro study, in vivo study, isotope labeling, molecular model, mouse, myocardial perfusion imaging, nonhuman, priority journal, radiochemistry, radioiodination, rat, room temperature, animal, blood, cardiac muscle, chemistry, computer simulation, diagnostic imaging, drug stability, heart, male, metabolism, myocardial perfusion imaging, procedures, statistics and numerical data, synthesis, tissue distribution, Animals, Computer Simulation, Drug Stability, Heart, In Vitro Techniques, Iodine Radioisotopes, Male, Mice, Models, Molecular, Myocardial Perfusion Imaging, Myocardium, Propanolamines, Radiopharmaceuticals, Rats, Receptors, Adrenergic, beta-1, Tissue Distribution