Preparation and molecular modeling of radioiodopropranolol as a novel potential radiopharmaceutical for lung perfusion scan
Keywords:
Radiopharmaceutiacls, Propranolol, 125I, Chloramine-T, Lung perfusion scan, Molecular modelingAbstract
Objective: Development of easy method for radioiodination of propranolol with high percent labeling yield for the purpose of lung perfusion imaging.
Methods: Radioidination of propranolol was achieved using 125I via electrophilic substitution under the oxidative conditions of cholramine-T (CAT). All factors affecting the labeling procedure and labeling yield were studied. Paper electrophoresis and HPLC were performed to determine the radiochemical yield and purity of the 125I-propranolol. Molecular modeling and docking studies were performed to ensure the binding of the newly obtained 125I-propranolol to beta-2 (β2) adrenergic receptor.
Results: Radioiodination of propranolol has been successfully achieved with high labeling yield (93.7 ± 0.81% ) . 125I-propranolol was stable for 24 h when kept in dark at ambient temperature. Biodistribution studies showed lung uptake of 21.60 ± 0.03% injected dose/g  (%ID/g) at 30 min post-injection. Molecular modeling confirmed that radioiodination did not affect the binding of propranolol to β2- receptor.
Conclusion: Iodopropranolol can be considered as good potential lung perfusion agent as suggested by the results of biodistribution and molecular modeling studies.
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References
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