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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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  <identifier identifierType="URL">https://zenodo.org/record/8581</identifier>
  <creators>
    <creator>
      <creatorName>Damont, Annelaure</creatorName>
      <givenName>Annelaure</givenName>
      <familyName>Damont</familyName>
      <affiliation>CEA, I2BM, Service Hospitalier Frédéric Joliot, 4 place du Général Leclerc, F-91406 Orsay, France</affiliation>
    </creator>
    <creator>
      <creatorName>Roeda, Dirk</creatorName>
      <givenName>Dirk</givenName>
      <familyName>Roeda</familyName>
      <affiliation>CEA, I2BM, Service Hospitalier Frédéric Joliot, 4 place du Général Leclerc, F-91406 Orsay, France</affiliation>
    </creator>
    <creator>
      <creatorName>Dollé, Frédéric</creatorName>
      <givenName>Frédéric</givenName>
      <familyName>Dollé</familyName>
      <affiliation>CEA, I2BM, Service Hospitalier Frédéric Joliot, 4 place du Général Leclerc, F-91406 Orsay, France</affiliation>
    </creator>
  </creators>
  <titles>
    <title>The potential of carbon-11 and fluorine-18 chemistry: Illustration through the development of PET-radioligands targeting the TSPO 18 kDa.</title>
  </titles>
  <publisher>Zenodo</publisher>
  <publicationYear>2013</publicationYear>
  <subjects>
    <subject>carbon-11</subject>
    <subject>fluorine-18</subject>
    <subject>PBR</subject>
    <subject>TSPO 18 kDa</subject>
    <subject>PET</subject>
  </subjects>
  <dates>
    <date dateType="Issued">2013-04-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://zenodo.org/record/8581</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1002/jlcr.2992</relatedIdentifier>
    <relatedIdentifier relatedIdentifierType="URL" relationType="IsPartOf">https://zenodo.org/communities/inmind</relatedIdentifier>
    <relatedIdentifier relatedIdentifierType="URL" relationType="IsPartOf">https://zenodo.org/communities/ecfunded</relatedIdentifier>
    <relatedIdentifier relatedIdentifierType="URL" relationType="IsPartOf">https://zenodo.org/communities/zenodo</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="info:eu-repo/semantics/closedAccess">Closed Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">&lt;p&gt;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&amp;#39;s, Parkinson&amp;#39;s and Huntington&amp;#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.&lt;/p&gt;</description>
  </descriptions>
  <fundingReferences>
    <fundingReference>
      <funderName>European Commission</funderName>
      <funderIdentifier funderIdentifierType="Crossref Funder ID">10.13039/501100000780</funderIdentifier>
      <awardNumber awardURI="info:eu-repo/grantAgreement/EC/FP7/278850/">278850</awardNumber>
      <awardTitle>Imaging of Neuroinflammation in Neurodegenerative Diseases</awardTitle>
    </fundingReference>
  </fundingReferences>
</resource>
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