Research output: Contribution to journal › Article
Alexandra Manos-Turvey, Guillaume Becker, Pierre Francotte, Maria Elisa Serrano, André Luxen, Bernard Pirotte, Alain Plenevaux, Christian Lemaire
Original language | English |
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Pages (from-to) | 788-795 |
Number of pages | 8 |
Journal | Chemmedchem |
Volume | 14 |
Issue number | 7 |
DOIs | |
Published | 3 Apr 2019 |
Alzheimer's disease (AD) remains a significant burden on society. In the search for new AD drugs, modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) are of particular interest, as loss of synaptic AMPARs has been linked to AD learning and memory deficits. Previously reported fluorine-containing BPAM121, an AMPA positive allosteric modulator (pam) with high activity, low toxicity, and slow metabolism, was considered to be a perfect 18 F-labeled candidate for positron emission tomography (PET) AD diagnostic investigations. For the preclinical use of this compound, an automated synthesis avoiding human radiation exposure was developed. The detailed production of [18 F]BPAM121 in relatively high quantity using a commercial FASTlab synthesizer from GE Healthcare coupled with a full set of quality controls is presented, along with procedures for the synthesis of the tosylated precursor and the fluorinated reference. To evaluate the clinical usefulness of [18 F]BPAM121 as a potential AD diagnostic, some in vivo studies in mice were then realized, alongside blocking and competition studies.
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