Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation

Sakr T.M.; Sanad M.H.; Abd-Alla W.H.; Salama D.H.; Saleh G.M.

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Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation

Sakr T.M.; Sanad M.H.; Abd-Alla W.H.; Salama D.H.; Saleh G.M.

Full Text link: https://t.ly/W5eg8

Date issued: 2018

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Doi: https://doi.org/10.1016/j.apradiso.2018.03.006 PubMed ID 29554644

Publisher: Elsevier Ltd

Series Info: Applied Radiation and Isotopes
137

Type: Article

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

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