Sakr T.M.Sanad M.H.Abd-Alla W.H.Salama D.H.Saleh G.M.Radioactive Isotopes and Generator DepartmentHot Labs CenterAtomic Energy AuthorityP.O. Box 13759CairoEgypt; Pharmaceutical Chemistry DepartmentFaculty of PharmacyOctober University of Modern Sciences and Arts (MSA)GizaEgypt; Labeled Compounds DepartmentHot Labs CenterAtomic Energy AuthorityP.O. Box 13759CairoEgypt; Pharmaceutical Chemistry DepartmentCollage of Pharmaceutical Science and Drug ManufacturingMisr University for Science & TechnologyP.O. 776th of October CityGizaEgypt; Health Radiation Research department (Radiodiagnosis Unit)National Center for Radiation Research and TechnologyAtomic Energy AuthorityCairoEgypt2020-01-092020-01-0920189698043https://doi.org/10.1016/j.apradiso.2018.03.006PubMed ID 29554644https://t.ly/W5eg8ScopusMSA Google ScholarChallenges 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 LtdEnglishOctober University for Modern Sciences and ArtsUniversity for Modern Sciences and ArtsMSA Universityجامعة أكتوبر للعلوم الحديثة والآدابCardiac imagingEsmololGamma scintigraphyMolecular modelingRadioiodinationMolecular modelingNuclear medicineAdrenergic receptorsCardiac imagingEsmololGamma scintigraphiesMolecular modeling studiesMyocardial perfusion imagingRadiochemical yieldRadioiodinationHeartbeta 1 adrenergic receptorcyanopindololdi iodinated esmololesmololmono iodinated esmololtracerunclassified drugbeta 1 adrenergic receptoresmololIodine-131propanolamine derivativeradioactive iodineradiopharmaceutical agentanimal experimentArticlecardioselectivitycomputer modeldrug receptor bindinggamma scintigraphyin vitro studyin vivo studyisotope labelingmolecular modelmousemyocardial perfusion imagingnonhumanpriority journalradiochemistryradioiodinationratroom temperatureanimalbloodcardiac musclechemistrycomputer simulationdiagnostic imagingdrug stabilityheartmalemetabolismmyocardial perfusion imagingproceduresstatistics and numerical datasynthesistissue distributionAnimalsComputer SimulationDrug StabilityHeartIn Vitro TechniquesIodine RadioisotopesMaleMiceModels, MolecularMyocardial Perfusion ImagingMyocardiumPropanolaminesRadiopharmaceuticalsRatsReceptors, Adrenergic, beta-1Tissue DistributionArticlehttps://doi.org/10.1016/j.apradiso.2018.03.006PubMed ID 29554644