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Special Issue "Current Aspects of Radiopharmaceutical Chemistry"

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

Deadline for manuscript submissions: closed (30 January 2018)

Special Issue Editor

Guest Editor
Prof. Dr. Peter Brust

Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstraße 15, 04318 Leipzig, Germany
Website | E-Mail
Interests: radiotracer development for brain tumor imaging (glioblastoma, brain metastases); neuroimaging of the cholinergic system (nicotinic acetylcholine receptors, vesicular acetylcholine transporter); neuroimaging of second messenger systems (phosphodiesterases 2, 5 and 10); neuroimaging of neuromodulatory processes (sigma and cannabinoid receptors, adenosine signaling); blood-brain barrier transport of radiopharmaceuticals

Special Issue Information

Dear Colleagues,

This Special Issue is related to recent developments in the field of radiopharmaceutical chemistry.

Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are in vivo molecular imaging devices which are widely used in nuclear medicine for diagnosis and treatment follow-up of many major diseases. They use biomolecules as probes, which are labeled with radionuclides of short half-lives, synthesized prior to the imaging studies. These probes are called radiopharmaceuticals. Their design and development is a rather interdisciplinary process covering many different disciplines of natural and health sciences. In addition to their diagnostic and therapeutic purposes in the field of nuclear medicine radiopharmaceuticals provide powerful tools for in vivo pharmacology during the process of pre-clinical drug development to identify new drug targets, to investigate the pathophysiology, to discover potential drug candidates, and to evaluate the pharmacokinetics and pharmacodynamics of drugs in vivo. Furthermore, they allow molecular imaging studies in various small-animal models of disease, including genetically engineered animals.

All researchers working in the field are cordially invited to contribute original research papers or reviews to this Special Issue of Molecules

Prof. Dr. Peter Brust
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 papers will be 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 monthly 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 1800 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

  • Radiolabelling
  • Radionuclide generators
  • Multimodality imaging probes
  • Carbon-11 chemistry
  • Fluorine-18 chemistry
  • Structure-based radiotracer design
  • Ligand-based radiotracer design
  • Target validation
  • Radiotracer metabolism
  • Neuroimaging
  • Tumor imaging

Published Papers (3 papers)

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Research

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Open AccessArticle Exploring the Metabolism of (+)-[18F]Flubatine in Vitro and in Vivo: LC-MS/MS Aided Identification of Radiometabolites in a Clinical PET Study
Molecules 2018, 23(2), 464; doi:10.3390/molecules23020464 (registering DOI)
Received: 29 January 2018 / Revised: 15 February 2018 / Accepted: 16 February 2018 / Published: 20 February 2018
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Abstract
Both (+)-[18F]flubatine and its enantiomer (−)-[18F]flubatine are radioligands for the neuroimaging of α4β2 nicotinic acetylcholine receptors (nAChRs) by positron emission tomography (PET). In a clinical study in patients with early Alzheimer’s disease, (+)-[18F]flubatine ((+)-[18F]1
[...] Read more.
Both (+)-[18F]flubatine and its enantiomer (−)-[18F]flubatine are radioligands for the neuroimaging of α4β2 nicotinic acetylcholine receptors (nAChRs) by positron emission tomography (PET). In a clinical study in patients with early Alzheimer’s disease, (+)-[18F]flubatine ((+)-[18F]1) was examined regarding its metabolic fate, in particular by identification of degradation products detected in plasma and urine. The investigations included an in vivo study of (+)-flubatine ((+)-1) in pigs and structural elucidation of formed metabolites by LC-MS/MS. Incubations of (+)-1 and (+)-[18F]1 with human liver microsomes were performed to generate in vitro metabolites, as well as radiometabolites, which enabled an assignment of their structures by comparison of LC-MS/MS and radio-HPLC data. Plasma and urine samples taken after administration of (+)-[18F]1 in humans were examined by radio-HPLC and, on the basis of results obtained in vitro and in vivo, formed radiometabolites were identified. Full article
(This article belongs to the Special Issue Current Aspects of Radiopharmaceutical Chemistry)
Figures

Open AccessArticle Synthesis of 11C-Labelled Ureas by Palladium(II)-Mediated Oxidative Carbonylation
Molecules 2017, 22(10), 1688; doi:10.3390/molecules22101688
Received: 25 September 2017 / Revised: 4 October 2017 / Accepted: 4 October 2017 / Published: 10 October 2017
PDF Full-text (3761 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Positron emission tomography is an imaging technique with applications in clinical settings as well as in basic research for the study of biological processes. A PET tracer, a biologically active molecule where a positron-emitting radioisotope such as carbon-11 has been incorporated, is used
[...] Read more.
Positron emission tomography is an imaging technique with applications in clinical settings as well as in basic research for the study of biological processes. A PET tracer, a biologically active molecule where a positron-emitting radioisotope such as carbon-11 has been incorporated, is used for the studies. Development of robust methods for incorporation of the radioisotope is therefore of the utmost importance. The urea functional group is present in many biologically active compounds and is thus an attractive target for incorporation of carbon-11 in the form of [11C]carbon monoxide. Starting with amines and [11C]carbon monoxide, both symmetrical and unsymmetrical 11C-labelled ureas were synthesised via a palladium(II)-mediated oxidative carbonylation and obtained in decay-corrected radiochemical yields up to 65%. The added advantage of using [11C]carbon monoxide was shown by the molar activity obtained for an inhibitor of soluble epoxide hydrolase (247 GBq/μmol–319 GBq/μmol). DFT calculations were found to support a reaction mechanism proceeding through an 11C-labelled isocyanate intermediate. Full article
(This article belongs to the Special Issue Current Aspects of Radiopharmaceutical Chemistry)
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Review

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Open AccessReview Advances in the Development of PET Ligands Targeting Histone Deacetylases for the Assessment of Neurodegenerative Diseases
Molecules 2018, 23(2), 300; doi:10.3390/molecules23020300
Received: 1 January 2018 / Revised: 29 January 2018 / Accepted: 29 January 2018 / Published: 31 January 2018
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Abstract
Epigenetic alterations of gene expression have emerged as a key factor in several neurodegenerative diseases. In particular, inhibitors targeting histone deacetylases (HDACs), which are enzymes responsible for deacetylation of histones and other proteins, show therapeutic effects in animal neurodegenerative disease models. However, the
[...] Read more.
Epigenetic alterations of gene expression have emerged as a key factor in several neurodegenerative diseases. In particular, inhibitors targeting histone deacetylases (HDACs), which are enzymes responsible for deacetylation of histones and other proteins, show therapeutic effects in animal neurodegenerative disease models. However, the details of the interaction between changes in HDAC levels in the brain and disease progression remain unknown. In this review, we focus on recent advances in development of radioligands for HDAC imaging in the brain with positron emission tomography (PET). We summarize the results of radiosynthesis and biological evaluation of the HDAC ligands to identify their successful results and challenges. Since 2006, several small molecules that are radiolabeled with a radioisotope such as carbon-11 or fluorine-18 have been developed and evaluated using various assays including in vitro HDAC binding assays and PET imaging in rodents and non-human primates. Although most compounds do not readily cross the blood-brain barrier, adamantane-conjugated radioligands tend to show good brain uptake. Until now, only one HDAC radioligand has been tested clinically in a brain PET study. Further PET imaging studies to clarify age-related and disease-related changes in HDACs in disease models and humans will increase our understanding of the roles of HDACs in neurodegenerative diseases. Full article
(This article belongs to the Special Issue Current Aspects of Radiopharmaceutical Chemistry)
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