18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands.
Org Biomol Chem
; 15(20): 4351-4358, 2017 May 23.
Article
en En
| MEDLINE
| ID: mdl-28474719
ABSTRACT
18F-Labelling of aromatic moieties was limited to electron deficient aromatic systems for many years but recent developments have provided access to the direct labelling of electron rich aromatic systems. Herein we report the synthesis and 18F-labelling of iodonium ylide precursors in the pursuit of 18F-labelled 5-HT2A receptor agonist PET-ligands. Subsequent evaluation in pigs showed high brain uptake of the PET ligands but a blocking dose of ketanserin did not significantly reduce the signal in relevant brain regions - indicating that the ligands do not interact specifically with the 5-HT2A receptor in vivo.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Radiofármacos
/
Receptor de Serotonina 5-HT2A
/
Tomografía de Emisión de Positrones
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Electrones
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Agonistas del Receptor de Serotonina 5-HT2
Límite:
Animals
Idioma:
En
Revista:
Org Biomol Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2017
Tipo del documento:
Article
País de afiliación:
Dinamarca