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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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    <subfield code="a">&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;</subfield>
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    <subfield code="a">Roeda, Dirk</subfield>
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    <subfield code="u">CEA, I2BM, Service Hospitalier Frédéric Joliot, 4 place du Général Leclerc, F-91406 Orsay, France</subfield>
    <subfield code="a">Dollé, Frédéric</subfield>
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