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In silico study and biological evaluation of 99mTc-tricabonyl oxiracetam as a selective imaging probe for AMPA receptors

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Abstract

The non-invasive quantification of AMPA receptors (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) could become a prognostic marker for brain disorders. 99mTc-tricarbonyl oxiracetam complex was prepared as a novel probe for AMPA receptor targeting with radiolabeling yield >98% and showed stability of 12 h. Molecular modeling and docking studies of 99mTc-tricarbonyl oxiracetam were performed. The results suggested that the complex act as very good positive allosteric modulators for AMPA receptor. The biodistribution studies revealed high brain uptake (7.5 ± 0.11% %ID/g) at 5 min post-I.V. injection that make 99mTc-tricarbonyl oxiracetam as a novel brain perfusion imaging radiotracer.

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Authors and Affiliations

  1. Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    M. H. Sanad

  2. Radioactive Isotopes and Generator Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    T. M. Sakr

  3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Misr University for Science & Technology, 6th of October City, Egypt

    Walaa H. A. Abdel-Hamid

  4. Biological Application Department, Nuclear Research Centre, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    E. A. Marzook

Authors
  1. M. H. Sanad
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  2. T. M. Sakr
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  3. Walaa H. A. Abdel-Hamid
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  4. E. A. Marzook
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Correspondence to M. H. Sanad.

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All institutional and national guidelines for the care and use of laboratory animals were followed. All authors declared no studies with human subjects.

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Sanad, M.H., Sakr, T.M., Abdel-Hamid, W.H.A. et al. In silico study and biological evaluation of 99mTc-tricabonyl oxiracetam as a selective imaging probe for AMPA receptors. J Radioanal Nucl Chem 314, 1505–1515 (2017). https://doi.org/10.1007/s10967-016-5120-y

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  • DOI: https://doi.org/10.1007/s10967-016-5120-y

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