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Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation.
- Source :
-
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2018 Jul; Vol. 137, pp. 41-49. Date of Electronic Publication: 2018 Mar 09. - Publication Year :
- 2018
-
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 β <subscript>1</subscript> -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 β <subscript>1</subscript> -adrenoceptor was confirmed by prior injection of cold esmolol. Gamma camera biodistribution pattern showed that radioiodinated esmolol accumulated selectively in heart.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Computer Simulation
Drug Stability
Heart diagnostic imaging
In Vitro Techniques
Male
Mice
Models, Molecular
Myocardial Perfusion Imaging statistics & numerical data
Myocardium metabolism
Rats
Receptors, Adrenergic, beta-1 metabolism
Tissue Distribution
Iodine Radioisotopes blood
Myocardial Perfusion Imaging methods
Propanolamines blood
Propanolamines chemical synthesis
Propanolamines chemistry
Radiopharmaceuticals blood
Radiopharmaceuticals chemical synthesis
Radiopharmaceuticals chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1872-9800
- Volume :
- 137
- Database :
- MEDLINE
- Journal :
- Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
- Publication Type :
- Academic Journal
- Accession number :
- 29554644
- Full Text :
- https://doi.org/10.1016/j.apradiso.2018.03.006