Browsing by Author "Saleh G.M."

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    Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation
    (Elsevier Ltd, 2018) Sakr T.M.; Sanad M.H.; Abd-Alla W.H.; Salama D.H.; Saleh G.M.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Collage of Pharmaceutical Science and Drug Manufacturing; Misr University for Science & Technology; P.O. 77; 6th of October City; Giza; Egypt; Health Radiation Research department (Radiodiagnosis Unit); National Center for Radiation Research and Technology; Atomic Energy Authority; Cairo; Egypt
    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