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Radiolabeling, docking studies, in silico ADME and biological evaluation of serotonin with 125I for 5-HTRs imaging

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Abstract

Serotonin is one of the significant signaling molecules used by several neural systems in the gut and brain. This study aimed to develop a novel and potent tracer for targeting, detecting, and imaging serotonin receptors (5-HTRs), which is a promising tool in the determination of the receptor’s function and relationship with the diseases related to serotonin and its receptor dysfunction. Serotonin was effectively labeled via a direct electrophilic substitutional reaction using an oxidizing agent such as iodogen with 125I in a neutral medium, and 125I-serotonin was achieved with a maximum labeling yield of 91 ± 0.63% with in vitro stability up to 24 h. Molecular modeling was conducted to signify 125I-serotonin structure and confirm that the radiolabeling process did not affect serotonin binding ability to its receptors. Biodistribution studies show that the maximum gastro intestinal tract uptake of 125I-serotonin was 17.8 ± 0.93% ID/organ after 30 min postinjection and the tracer’s ability to pass the blood–brain barrier. Thus, 125 I-serotonin is a promising single photon emission computed tomography tracer in the detection of 5HTRs.

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Authors and Affiliations

  1. Labeled Compounds Department, Hot Lab. Center, Egyptian Atomic Energy Authority (EAEA), P.O. Box 13759, Cairo, Egypt

    Dina M. El-Sharawy & H. Hussien

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

    Marwa S. El Refaye

  3. Cyclotron Project, Nuclear Research Center, Cairo, Egypt

    Dina M. El-Sharawy, Marwa S. El Refaye & H. Hussien

  4. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University, Beni Suef, Egypt

    Asmaa M. AboulMagd

  5. Pharmaceutics and Clinical Pharmacy Department, Faculty of Pharmacy, Nahda University, Beni Suef, Egypt

    Dina M. El-Sharawy

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  1. Dina M. El-Sharawy
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  2. Marwa S. El Refaye
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  3. H. Hussien
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  4. Asmaa M. AboulMagd
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Correspondence to Dina M. El-Sharawy or Asmaa M. AboulMagd.

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El-Sharawy, D.M., Refaye, M.S.E., Hussien, H. et al. Radiolabeling, docking studies, in silico ADME and biological evaluation of serotonin with 125I for 5-HTRs imaging. NUCL SCI TECH 31, 80 (2020). https://doi.org/10.1007/s41365-020-00784-9

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  • DOI: https://doi.org/10.1007/s41365-020-00784-9

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