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Molecules
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Novel Radiopharmaceuticals for PET and SPECT Imaging
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Novel Radiopharmaceuticals for PET and SPECT Imaging

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 1915

Special Issue Editor

Dr. James C Knight

E-Mail Website
Guest Editor
School of Natural and Environmental Sciences, Newcastle University, Newcastle upon Tyne NE1 7RU, UK
Interests: radiochemistry; PET imaging; cancer research; theranostics; molecular imaging

Special Issue Information

Dear Colleagues,

Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are important imaging techniques in the era of personalized medicine. Both PET and SPECT rely on radiotracers to probe specific biomarkers of disease with exquisite sensitivity, and the resulting images can help guide patient management and improve clinical outcomes. At present, only a very small selection of PET and SPECT radiotracers are used routinely in clinical settings but this is primed for expansion as recent advances in molecular pathology have revealed a wide array of attractive imaging biomarkers for several disease states. This expansion will be facilitated by recent developments in radiochemistry that have provided efficient synthetic routes to hitherto inaccessible radiotracers and also helped foster exciting innovations in probe design. The aim of this Special Issue is to collate examples of novel PET and SPECT radiotracers that have the potential to advance this important medical frontier.

Dr. James C Knight
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • radiochemistry
  • positron emission tomography
  • single-photon emission computed tomography
  • radiotracers
  • radioligands
  • radiopharmaceuticals
  • molecular imaging
  • early detection
  • monitoring therapy
  • personalized medicine

Published Papers (1 paper)

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Research

17 pages, 3698 KiB  
Article
[124I]IBETA: A New Aβ Plaque Positron Emission Tomography Imaging Agent for Alzheimer’s Disease
by Grace A.H. Nguyen, Christopher Liang and Jogeshwar Mukherjee
Molecules 2022, 27(14), 4552; https://doi.org/10.3390/molecules27144552 - 17 Jul 2022
Cited by 12 | Viewed by 1723
Abstract
Several fluorine-18-labeled PET β-amyloid (Aβ) plaque radiotracers for Alzheimer’s disease (AD) are in clinical use. However, no radioiodinated imaging agent for Aβ plaques has been successfully moved forward for either single-photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. Radioiodinated pyridyl [...] Read more.
Several fluorine-18-labeled PET β-amyloid (Aβ) plaque radiotracers for Alzheimer’s disease (AD) are in clinical use. However, no radioiodinated imaging agent for Aβ plaques has been successfully moved forward for either single-photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. Radioiodinated pyridyl benzofuran derivatives for the SPECT imaging of Aβ plaques using iodine-123 and iodine-125 are being pursued. In this study, we assess the iodine-124 radioiodinated pyridyl benzofuran derivative 5-(5-[124I]iodobenzofuran-2-yl)-N,N-dimethylpyridin-2-amine ([124I]IBETA) (Ki = 2.36 nM) for utilization in PET imaging for Aβ plaques. We report our findings on the radioiododestannylation reaction used to prepare [124/125I]IBETA and evaluate its binding to Aβ plaques in a 5 × FAD mouse model and postmortem human AD brain. Both [125I]IBETA and [124I]IBETA are produced in >25% radiochemical yield and >85% radiochemical purity. The in vitro binding of [125I]IBETA and [124I]IBETA in transgenic 5 × FAD mouse model for Aβ plaques was high in the frontal cortex, anterior cingulate, thalamus, and hippocampus, which are regions of high Aβ accumulation, with very little binding in the cerebellum (ratio of brain regions to cerebellum was >5). The in vitro binding of [125I]IBETA and [124I]IBETA in postmortem human AD brains was higher in gray matter containing Aβ plaques compared to white matter (ratio of gray to white matter was >5). Anti-Aβ immunostaining strongly correlated with [124/125I]IBETA regional binding in both the 5 × FAD mouse and postmortem AD human brains. The binding of [124/125I]IBETA in 5 × FAD mouse and postmortem human AD brains was displaced by the known Aβ plaque imaging agent, Flotaza. Preliminary PET/CT studies of [124I]IBETA in the 5 × FAD mouse model suggested [124I]IBETA was relatively stable in vivo with a greater localization of [124I]IBETA in the brain regions with a high concentration of Aβ plaques. Some deiodination was observed at later time points. Therefore, [124I]IBETA may potentially be a useful PET radioligand for Aβ plaques in brain studies. Full article
(This article belongs to the Special Issue Novel Radiopharmaceuticals for PET and SPECT Imaging)
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