PREPARATION AND MOLECULAR MODELING OF RADIOIODOPROPRANOLOL AS A NOVEL POTENTIAL RADIOPHARMACEUTICAL FOR LUNG PERFUSION SCAN (original) (raw)

Objective: Development of an easy method for radio iodination of propranolol with high percent labeling yield for the purpose of lung perfusion imaging. Methods: Radioidination of propranolol was achieved using 125 I 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 125 I-propranolol. Biodistribution studies were performed to determine the lung deposition of iodo propranolol by injecting the labeled propranolol into the tail vein of Swiss Albino mice. Molecular modeling and docking studies were performed to ensure the binding of the newly obtained 125 I-propranolol to beta-2 (β2) adrenergic receptor. Results: Radioiodination of propranolol has been successfully achieved with a high labeling yield (93.7±0.81%). 125 I-propranolol was stable for 24 h when kept away from light, 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 radio iodination 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. INTRODUCTION Nuclear medicine imaging, non-invasively provides functional information at the molecular and cellular level that contributes to the determination of health status by measuring the uptake and turnover of target specific radiotracers in tissues [1].

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