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Radioiodination and biological evaluation of salbutamol as a β2-adrenoceptor agonist

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Abstract

A procedure for preparing high-radiochemical-purity 125I-salbutamol was developed in order to characterize the binding properties of β2-adrenoceptors. Direct radioiodination of salbutamol was carried out using Chloramine T as an oxidizing agent. The optimized conditions for salbutamol labeling with 125I are as follows: 100 μg of salbutamol, 50 μg of Chloramine T, 150 μl of phosphate buffer (pH 7), room temperature (25 ± 1°C), 5 min. The radiochemical yield of up to 98% was attained. The radiochemical yield and purity of the labeled product were evaluated by electrophoresis and HPLC. Biodistribution studies were carried out in normal Albino Swiss mice at different time intervals after administration of 125I-salbutamol. The results indicate that the labeled compound cleared from the systematic circulation within 3 h after administration and majority of organs showed significant decrease in the 125I-salbutamol uptake. The heart and lung uptake was high. 125I-Salbutamol can be used as β-receptor imaging agent.

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Authors and Affiliations

  1. Labelled Compounds Department, Radioisotopes Production and Radioactive Sources Division, Hot Laboratories Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    M. El-Tawoosy & I. T. Ibrahim

Authors
  1. M. El-Tawoosy
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  2. I. T. Ibrahim
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Correspondence to M. El-Tawoosy.

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Published in Russian in Radiokhimiya, 2012, Vol. 54, No. 4, pp. 369–373.

The text was submitted by the authors in English.

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El-Tawoosy, M., Ibrahim, I.T. Radioiodination and biological evaluation of salbutamol as a β2-adrenoceptor agonist. Radiochemistry 54, 401–406 (2012). https://doi.org/10.1134/S1066362212040169

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  • DOI: https://doi.org/10.1134/S1066362212040169

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