Preparation and molecular modeling of radioiodopropranolol as a novel potential radiopharmaceutical for lung perfusion scan

  • Mohammed A. El-motaleb Labeled Compounds Department, Hot Lab. Center, Atomic Energy Authority,
  • Amal S. Farrag Pharmaceutical Chemistry Dept. Faculty of Pharmacy, AL-Azher University
  • Ismail T. Ibrahim Labeled Compounds Department, Hot Lab. Center, Atomic Energy Authority,
  • Mona O. Sarhan Labeled Compounds Department, Hot Lab. Center, Atomic Energy Authority,
  • Magda F. Ismail Pharmaceutical Chemistry Dept. Faculty of Pharmacy, AL-Azher University

Abstract

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.

Keywords: Radiopharmaceutiacls, Propranolol, 125I, Chloramine-T, Lung perfusion scan, Molecular modeling

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Author Biography

Mona O. Sarhan, Labeled Compounds Department, Hot Lab. Center, Atomic Energy Authority,
Department of Labeled compounds, Hot Lab center

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How to Cite
El-motaleb, M. A., A. S. Farrag, I. T. Ibrahim, M. O. Sarhan, and M. F. Ismail. “Preparation and Molecular Modeling of Radioiodopropranolol As a Novel Potential Radiopharmaceutical for Lung Perfusion Scan”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 8, no. 8, June 2015, pp. 110-6, https://innovareacademics.in/journals/index.php/ijpps/article/view/5018.
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