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Rigshospitalet - en del af Københavns Universitetshospital
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Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [(18) F]Cimbi-92 and [(18) F]Cimbi-150

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DOI

  1. Radiosynthesis and preclinical evaluation of [11 C]Cimbi-701 - Towards the imaging of cerebral 5-HT7 receptors

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  2. Evaluation of [18 F]2FP3 in pigs and non-human primates

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  3. Current radiosynthesis strategies for 5-HT2A receptor PET tracers

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  1. A Single Dose of Psilocybin Increases Synaptic Density and Decreases 5-HT2A Receptor Density in the Pig Brain

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  2. Effects of a single dose of psilocybin on behaviour, brain 5-HT2A receptor occupancy and gene expression in the pig

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  3. Plasma psilocin critically determines behavioral and neurobiological effects of psilocybin

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  4. Imaging of the Serotonin System: Radiotracers and Applications in Memory Disorders

    Publikation: Bidrag til bog/antologi/rapportBidrag til bog/antologiUndervisning

  5. Metaboliske, endokrine og andre systemiske sygdomme

    Publikation: Bidrag til bog/antologi/rapportBidrag til bog/antologiUndervisning

Vis graf over relationer

An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [(11) C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an (18) F-labelled agonist 5-HT2A receptor (5-HT2A R) tracer is highly sought after. Herein, we report a 2-step, 1-pot labelling methodology of 2 tracer candidates. Both ligands display high in vitro affinities for the 5-HT2A R. The compounds were synthesised from easily accessible labelling precursors, and radiolabelled in acceptable radiochemical yields, sufficient for in vivo studies in domestic pigs. PET images partially conformed to the expected brain distribution of the 5-HT2A R; a notable exception however being significant uptake in the striatum and thalamus. Additionally, a within-scan displacement challenge with a 5-HT2A R antagonist was unsuccessful, indicating that the tracers cannot be considered optimal for neuroimaging of the 5-HT2A R.

OriginalsprogEngelsk
TidsskriftJournal of Labelled Compounds and Radiopharmaceuticals
Vol/bind60
Udgave nummer12
Sider (fra-til)586-591
Antal sider6
ISSN0362-4803
DOI
StatusUdgivet - okt. 2017

ID: 52018814