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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", 
  "container_title": "J Labelled Comp Radiopharm.", 
  "title": "The potential of carbon-11 and fluorine-18 chemistry: Illustration through the development of PET-radioligands targeting the TSPO 18 kDa.", 
  "issued": {
    "date-parts": [
      [
        2013, 
        4, 
        1
      ]
    ]
  }, 
  "abstract": "<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>", 
  "author": [
    {
      "given": "Annelaure", 
      "family": "Damont"
    }, 
    {
      "given": "Dirk", 
      "family": "Roeda"
    }, 
    {
      "given": "Fr\u00e9d\u00e9ric", 
      "family": "Doll\u00e9"
    }
  ], 
  "page": "96-104", 
  "volume": "56", 
  "type": "article-journal", 
  "issue": "3-4", 
  "id": "8581"
}
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