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Optimization and tissue distribution of [125I]iododomperidone as a radiotracer for D2-receptor imaging

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Abstract

The aim of the present study is to use [125I]iododomperidone (125I-DOM) as a novel radioligand for dopamine D2-receptor (D2R) imaging. Therefore, a 12 h in vitro stable [125I]iododomperidone was synthesized with a maximum radiochemical yield (RCY) of 95.5% in subsistence of chloramine-T (CAT) as an oxidant. Furthermore, molecular operating environment (MOE) design was employed to assess the determination of the [125I]iododomperidone structure. The product structure was confirmed by employing cold iodination reaction using iodine-127. Moreover, the computational data which obtained from PreADMET software proved the increase of lipophilicity of [125I]iododomperidone over that of unlabeled one. In a trial to confirm the targeting ability of [125I]iododomperidone to D2R, docking study was performed and showed a successful binding of the labeled compound to the receptor. The biodistribution profile of [125I]iododomperidone in normal mice showed a rapid and high uptake of the brain (5.6 ± 0.2% ID/g organ) at 5 min post injection (p.i.). Consequently, [125I]iododomperidone will be a potential unprecedented D2R imaging agent for diagnosis of various neuropsychiatric disorders.

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Acknowledgements

The authors would like to acknowledge Dr. Asmaa M. AboulMagd, Lecturer of Pharmaceutical Chemistry, Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University in Beni Sueif (NUB), for her contribution in the use of MOE and PreADMET softwares. The authors would like to thank Dr. A. M. Rashad, Central Laboratory for Elemental and Isotopic Analysis, Nuclear Research Center, Atomic Energy Authority, Cairo, Egypt, for his contribution in docking study.

Funding

Moreover, this research did not receive any specific grant from funding agencies in the public, commercial or not-for-profit sectors.

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Authors and Affiliations

  1. Cyclotron Project, Nuclear Research Centre, Egyptian Atomic Energy Authority (EAEA), B.O. 13759, Cairo, Egypt

    S. I. Khater, Dina M. El-Sharawy & Marwa S. El Refaye

  2. Radioactive Isotopes and Generators Department, Hot Lab. Center, Egyptian Atomic Energy Authority (EAEA), B.O. 13759, Cairo, Egypt

    S. I. Khater & Marwa S. El Refaye

  3. Labeled Compounds Department, Hot Lab. Center, Egyptian Atomic Energy Authority (EAEA), B.O. 13759, Cairo, Egypt

    Dina M. El-Sharawy & Nourihan S. Farrag

  4. Pharmaceutics and Clinical Pharmacy Department, Faculty of Pharmacy, Nahda University (NUB), Beni-Sweif, Egypt

    Dina M. El-Sharawy

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  1. S. I. Khater
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  2. Dina M. El-Sharawy
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  3. Marwa S. El Refaye
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  4. Nourihan S. Farrag
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Correspondence to Nourihan S. Farrag.

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Khater, S.I., El-Sharawy, D.M., El Refaye, M.S. et al. Optimization and tissue distribution of [125I]iododomperidone as a radiotracer for D2-receptor imaging. J Radioanal Nucl Chem 325, 343–355 (2020). https://doi.org/10.1007/s10967-020-07236-z

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  • DOI: https://doi.org/10.1007/s10967-020-07236-z

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