Article (Scientific journals)
Fully Automated Synthesis and Evaluation of [ 18 F]BPAM121: Potential of an AMPA Receptor Positive Allosteric Modulator as PET Radiotracer
Manos-Turvey, A.; Becker, Guillaume; Francotte, Pierre et al.
2019In ChemMedChem, 14 (7), p. 788-795
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Keywords :
AMPA receptors; BPAM; fluorine 18
Abstract :
[en] 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. © 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
Disciplines :
Radiology, nuclear medicine & imaging
Author, co-author :
Manos-Turvey, A.;  CIRM, Laboratoire de Chimie Pharmaceutique, Université de Liège, Quartier Hopital, Avenue Hippocrate 15, Liège, 4000, Belgium, Bayer AG, Crop Science Division, Industriepark Höchst G836, Frankfurt am Main, 65926, Germany
Becker, Guillaume ;  Université de Liège - ULiège > Département de Psychologie > Département de Psychologie
Francotte, Pierre  ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Serrano Navacerrada, Maria Elisa ;  Université de Liège - ULiège > CRC In vivo Imaging-Preclinical Imaging
Luxen, André ;  Université de Liège - ULiège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse
Pirotte, Bernard ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Plenevaux, Alain  ;  Université de Liège - ULiège > Département de chimie (sciences) > Département de chimie (sciences)
Lemaire, Christian ;  Université de Liège - ULiège > CRC In vivo Imaging-Radiochemistry
Language :
English
Title :
Fully Automated Synthesis and Evaluation of [ 18 F]BPAM121: Potential of an AMPA Receptor Positive Allosteric Modulator as PET Radiotracer
Publication date :
11 February 2019
Journal title :
ChemMedChem
ISSN :
1860-7179
eISSN :
1860-7187
Publisher :
John Wiley and Sons Ltd
Volume :
14
Issue :
7
Pages :
788-795
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique
Available on ORBi :
since 27 May 2019

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