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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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{
  "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>", 
  "creator": [
    {
      "affiliation": "CEA, I2BM, Service Hospitalier Fr\u00e9d\u00e9ric Joliot, 4 place du G\u00e9n\u00e9ral Leclerc, F-91406 Orsay, France", 
      "@type": "Person", 
      "name": "Damont, Annelaure"
    }, 
    {
      "affiliation": "CEA, I2BM, Service Hospitalier Fr\u00e9d\u00e9ric Joliot, 4 place du G\u00e9n\u00e9ral Leclerc, F-91406 Orsay, France", 
      "@type": "Person", 
      "name": "Roeda, Dirk"
    }, 
    {
      "affiliation": "CEA, I2BM, Service Hospitalier Fr\u00e9d\u00e9ric Joliot, 4 place du G\u00e9n\u00e9ral Leclerc, F-91406 Orsay, France", 
      "@type": "Person", 
      "name": "Doll\u00e9, Fr\u00e9d\u00e9ric"
    }
  ], 
  "headline": "The potential of carbon-11 and fluorine-18 chemistry: Illustration through the development of PET-radioligands targeting the TSPO 18 kDa.", 
  "image": "https://zenodo.org/static/img/logos/zenodo-gradient-round.svg", 
  "datePublished": "2013-04-01", 
  "url": "https://zenodo.org/record/8581", 
  "keywords": [
    "carbon-11", 
    "fluorine-18", 
    "PBR", 
    "TSPO 18 kDa", 
    "PET"
  ], 
  "@context": "https://schema.org/", 
  "identifier": "https://doi.org/10.1002/jlcr.2992", 
  "@id": "https://doi.org/10.1002/jlcr.2992", 
  "@type": "ScholarlyArticle", 
  "name": "The potential of carbon-11 and fluorine-18 chemistry: Illustration through the development of PET-radioligands targeting the TSPO 18 kDa."
}
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