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The potential of carbon-11 and fluorine-18 chemistry: Illustration through the development of PET-radioligands targeting the TSPO 18 kDa.

Damont, Annelaure; Roeda, Dirk; Dollé, Frédéric


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  "doi": "10.1002/jlcr.2992", 
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  "metadata": {
    "access_right_category": "danger", 
    "doi": "10.1002/jlcr.2992", 
    "description": "<p>The TSPO (translocator protein), also known as the peripheral benzodiazepine receptor, is upregulated in the brain of subjects suffering from neurodegenerative disorders such as Alzheimer&#39;s, Parkinson&#39;s and Huntington&#39;s disease. Moreover, this overexpression has been proved to be linked to microglia activation making thus the TSPO a marker of choice of neuroinflammatory processes and therefore a potential target for the development of radioligands for positron emission tomography imaging. The discovery of selective TSPO ligands and their labelling with the short-lived positron-emitter isotopes carbon-11 and fluorine-18 emerged in the mid-1980s with the preparation of the 3-isoquinolinecarboxamide [(11) C]PK11195. To date, an impressive number of promising compounds-[(11) C]PK11195-challengers-have been developed; some radioligands-for example, [(11) C]PBR28, [(11) C]DPA-713, [(18) F]FEDAA1106 and [(18) F]DPA-714-are currently used in clinical trials. As illustrated in this review, the methodologies applied for the preparation of these compounds remain mainly [(11) C]methylations using [(11) C]MeI or [(11) C]MeOTf and SN 2-type nucleophilic aliphatic [(18) F]fluorinations-two processes illustrating the state-of-the-art arsenal of reactions that involves these two short-lived radioisotopes-but alternative processes, such as [(11) C]carbonylations using [(11) C]CO and [(11) C]COCl2 as well as SN Ar-type nucleophilic [(18) F]fluorinations, have also been reported and as such, reviewed herein.</p>", 
    "title": "The potential of carbon-11 and fluorine-18 chemistry: Illustration through the development of PET-radioligands targeting the TSPO 18 kDa.", 
    "journal": {
      "volume": "56", 
      "year": "2013", 
      "issue": "3-4", 
      "pages": "96-104", 
      "title": "J Labelled Comp Radiopharm."
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        "code": "278850", 
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        "title": "Imaging of Neuroinflammation in Neurodegenerative Diseases", 
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    "keywords": [
      "carbon-11", 
      "fluorine-18", 
      "PBR", 
      "TSPO 18 kDa", 
      "PET"
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    "publication_date": "2013-04-01", 
    "creators": [
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        "affiliation": "CEA, I2BM, Service Hospitalier Fr\u00e9d\u00e9ric Joliot, 4 place du G\u00e9n\u00e9ral Leclerc, F-91406 Orsay, France", 
        "name": "Damont, Annelaure"
      }, 
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        "affiliation": "CEA, I2BM, Service Hospitalier Fr\u00e9d\u00e9ric Joliot, 4 place du G\u00e9n\u00e9ral Leclerc, F-91406 Orsay, France", 
        "name": "Roeda, Dirk"
      }, 
      {
        "affiliation": "CEA, I2BM, Service Hospitalier Fr\u00e9d\u00e9ric Joliot, 4 place du G\u00e9n\u00e9ral Leclerc, F-91406 Orsay, France", 
        "name": "Doll\u00e9, Fr\u00e9d\u00e9ric"
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