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

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorSakr T.M.
dc.contributor.authorSanad M.H.
dc.contributor.authorAbd-Alla W.H.
dc.contributor.authorSalama D.H.
dc.contributor.authorSaleh G.M.
dc.contributor.otherRadioactive Isotopes and Generator Department
dc.contributor.otherHot Labs Center
dc.contributor.otherAtomic Energy Authority
dc.contributor.otherP.O. Box 13759
dc.contributor.otherCairo
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University of Modern Sciences and Arts (MSA)
dc.contributor.otherGiza
dc.contributor.otherEgypt; Labeled Compounds Department
dc.contributor.otherHot Labs Center
dc.contributor.otherAtomic Energy Authority
dc.contributor.otherP.O. Box 13759
dc.contributor.otherCairo
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherCollage of Pharmaceutical Science and Drug Manufacturing
dc.contributor.otherMisr University for Science & Technology
dc.contributor.otherP.O. 77
dc.contributor.other6th of October City
dc.contributor.otherGiza
dc.contributor.otherEgypt; Health Radiation Research department (Radiodiagnosis Unit)
dc.contributor.otherNational Center for Radiation Research and Technology
dc.contributor.otherAtomic Energy Authority
dc.contributor.otherCairo
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:40:54Z
dc.date.available2020-01-09T20:40:54Z
dc.date.issued2018
dc.descriptionScopus
dc.descriptionMSA Google Scholar
dc.description.abstractChallenges 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 Ltden_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=40907&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1016/j.apradiso.2018.03.006
dc.identifier.doiPubMed ID 29554644
dc.identifier.issn9698043
dc.identifier.otherhttps://doi.org/10.1016/j.apradiso.2018.03.006
dc.identifier.otherPubMed ID 29554644
dc.identifier.urihttps://t.ly/W5eg8
dc.language.isoEnglishen_US
dc.publisherElsevier Ltden_US
dc.relation.ispartofseriesApplied Radiation and Isotopes
dc.relation.ispartofseries137
dc.subjectOctober University for Modern Sciences and Arts
dc.subjectUniversity for Modern Sciences and Arts
dc.subjectMSA University
dc.subjectجامعة أكتوبر للعلوم الحديثة والآداب
dc.subjectCardiac imagingen_US
dc.subjectEsmololen_US
dc.subjectGamma scintigraphyen_US
dc.subjectMolecular modelingen_US
dc.subjectRadioiodinationen_US
dc.subjectMolecular modelingen_US
dc.subjectNuclear medicineen_US
dc.subjectAdrenergic receptorsen_US
dc.subjectCardiac imagingen_US
dc.subjectEsmololen_US
dc.subjectGamma scintigraphiesen_US
dc.subjectMolecular modeling studiesen_US
dc.subjectMyocardial perfusion imagingen_US
dc.subjectRadiochemical yielden_US
dc.subjectRadioiodinationen_US
dc.subjectHearten_US
dc.subjectbeta 1 adrenergic receptoren_US
dc.subjectcyanopindololen_US
dc.subjectdi iodinated esmololen_US
dc.subjectesmololen_US
dc.subjectmono iodinated esmololen_US
dc.subjecttraceren_US
dc.subjectunclassified drugen_US
dc.subjectbeta 1 adrenergic receptoren_US
dc.subjectesmololen_US
dc.subjectIodine-131en_US
dc.subjectpropanolamine derivativeen_US
dc.subjectradioactive iodineen_US
dc.subjectradiopharmaceutical agenten_US
dc.subjectanimal experimenten_US
dc.subjectArticleen_US
dc.subjectcardioselectivityen_US
dc.subjectcomputer modelen_US
dc.subjectdrug receptor bindingen_US
dc.subjectgamma scintigraphyen_US
dc.subjectin vitro studyen_US
dc.subjectin vivo studyen_US
dc.subjectisotope labelingen_US
dc.subjectmolecular modelen_US
dc.subjectmouseen_US
dc.subjectmyocardial perfusion imagingen_US
dc.subjectnonhumanen_US
dc.subjectpriority journalen_US
dc.subjectradiochemistryen_US
dc.subjectradioiodinationen_US
dc.subjectraten_US
dc.subjectroom temperatureen_US
dc.subjectanimalen_US
dc.subjectblooden_US
dc.subjectcardiac muscleen_US
dc.subjectchemistryen_US
dc.subjectcomputer simulationen_US
dc.subjectdiagnostic imagingen_US
dc.subjectdrug stabilityen_US
dc.subjecthearten_US
dc.subjectmaleen_US
dc.subjectmetabolismen_US
dc.subjectmyocardial perfusion imagingen_US
dc.subjectproceduresen_US
dc.subjectstatistics and numerical dataen_US
dc.subjectsynthesisen_US
dc.subjecttissue distributionen_US
dc.subjectAnimalsen_US
dc.subjectComputer Simulationen_US
dc.subjectDrug Stabilityen_US
dc.subjectHearten_US
dc.subjectIn Vitro Techniquesen_US
dc.subjectIodine Radioisotopesen_US
dc.subjectMaleen_US
dc.subjectMiceen_US
dc.subjectModels, Molecularen_US
dc.subjectMyocardial Perfusion Imagingen_US
dc.subjectMyocardiumen_US
dc.subjectPropanolaminesen_US
dc.subjectRadiopharmaceuticalsen_US
dc.subjectRatsen_US
dc.subjectReceptors, Adrenergic, beta-1en_US
dc.subjectTissue Distributionen_US
dc.titleRadioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluationen_US
dc.typeArticleen_US
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