18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands
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18F-Labelling of electron rich iodonium ylides : application to the radiosynthesis of potential 5-HT2A receptor PET ligands. / Petersen, I N; Villadsen, J; Hansen, H D; Madsen, J; Jensen, A A; Gillings, N; Lehel, Szabolcs; Herth, M M; Knudsen, G M; Kristensen, J L.
In: Organic & Biomolecular Chemistry, Vol. 15, 04.2017, p. 4351-4358.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - 18F-Labelling of electron rich iodonium ylides
T2 - application to the radiosynthesis of potential 5-HT2A receptor PET ligands
AU - Petersen, I N
AU - Villadsen, J
AU - Hansen, H D
AU - Madsen, J
AU - Jensen, A A
AU - Gillings, N
AU - Lehel, Szabolcs
AU - Herth, M M
AU - Knudsen, G M
AU - Kristensen, J L
PY - 2017/4
Y1 - 2017/4
N2 - (18)F-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 (18)F-labelling of iodonium ylide precursors in the pursuit of (18)F-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.
AB - (18)F-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 (18)F-labelling of iodonium ylide precursors in the pursuit of (18)F-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.
KW - Journal Article
U2 - 10.1039/c7ob00628d
DO - 10.1039/c7ob00628d
M3 - Journal article
C2 - 28474719
VL - 15
SP - 4351
EP - 4358
JO - Organic & Biomolecular Chemistry
JF - Organic & Biomolecular Chemistry
SN - 1470-4358
ER -
ID: 177414505