Poster (Scientific congresses and symposiums)
Design and Synthesis of [18F]BPAM121, a PET-Probe Targeting AMPA-subtype Glutamatergic Receptors.
Manos-Turvey, Alexandra; Lemaire, Christian; Becker, Guillaume et al.
2017EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry
 

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Keywords :
AMPA; PET probe; Alzheimer's disease
Abstract :
[en] AMPA receptors (AMPARs), one of three sub-groups of ionotropic glutamate receptors present in the central nervous system, are recognised for their involvement in long-term potentiation (LTP), and learning and memory processes. [1] They represent a valid cognitive enhancer target, particularly in the fight against Alzheimer’s disease (AD). [2,3] Benzothiadiazine 1,1-dioxides, such as BPAM121, have emerged as important allosteric modulators of AMPARs, working solely in the presence of the endogenous transmitter. [4] Synthesis of BPAM121 labelled with fluorine-18 was proposed, to investigate the utility of this molecule as a PET probe in vivo, and evaluate its potential as an AD diagnostic tool (Figure 1). [Figure 1. a) Structure of BPAM121, b) Established radiochemical synthesis of [18F]BPAM121.] This work documents the successful optimization of synthesis, purification and formulation of [18F]BPAM121 using an automated FASTlab (GE Healthcare) synthesizer. In particular, the influence of higher-level [18F]fluoride ion starting concentrations on final product formulation requirements is discussed. Initial results revealed [18F]BPAM121 successfully passes the blood brain barrier, and further biological studies are currently underway. References [1] S. F. Traynelis et al. Pharmacol. Rev. 2010, 62, 405-496. 
 [2] J. Keifer, Z. Zheng, Eur. J. Neurosci. 2010, 32, 269-277. 
 [3] L. Gao et al. J. Neurochem. 2016, 136, 620-636. 
 [4] P. Francotte et al. J. Med. Chem. 2010, 53, 1700-1711. 

Research center :
CIRM - Centre Interdisciplinaire de Recherche sur le Médicament - ULiège
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Manos-Turvey, Alexandra ;  Université de Liège > Département de pharmacie > Chimie pharmaceutique
Lemaire, Christian ;  Université de Liège > Centre de recherches du cyclotron
Becker, Guillaume ;  Université de Liège > Centre de recherches du cyclotron
Plenevaux, Alain  ;  Université de Liège > Département de chimie (sciences) > Département de chimie (sciences)
Luxen, André ;  Université de Liège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse
Pirotte, Bernard ;  Université de Liège > Département de pharmacie > Chimie pharmaceutique
Francotte, Pierre  ;  Université de Liège > Département de pharmacie > Chimie pharmaceutique
Language :
English
Title :
Design and Synthesis of [18F]BPAM121, a PET-Probe Targeting AMPA-subtype Glutamatergic Receptors.
Publication date :
August 2017
Number of pages :
A0
Event name :
EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry
Event organizer :
EFMC
Event place :
Vienne, Austria
Event date :
27-31 août 2017
Audience :
International
Funders :
Fonds Léon Fredericq [BE]
Marie Curie BeIPD-COFUND / European Commission
ULiège - Université de Liège [BE]
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
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since 07 September 2017

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