Article (Scientific journals)
Pharmacokinetic characterization of [18F]UCB-H PET radiopharmaceutical in the rat brain.
Becker, Guillaume; Warnier, Corentin; Serrano Navacerrada, Maria Elisa et al.
2017In Molecular Pharmaceutics, 14 (8), p. 2719-2725
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Keywords :
SV2A; [18F]UCB-H; PET; chirality; population-based input function
Abstract :
[en] The synaptic vesicle glycoprotein 2A (SV2A), a protein essential to the proper nervous system function, is found in presynaptic vesicles. Thus, SV2A targeting, using dedicated radiotracers combined with positron emission tomography (PET), allows the assessment of synaptic density in the living brain. The first-in-class fluorinated SV2A specific radioligand, [18F]UCB-H, is now available at high-activity through an efficient radiosynthesis compliant with the current good manufacturing practices (cGMP). We report here a non-invasive method to quantify [18F]UCB-H binding in rat brain with microPET. Validation study in rats confirmed the need of high enantiomeric purity to target SV2A in vivo. We demonstrated the reliability of a population-based input function to quantify SV2A in preclinical microPET setting. Finally, we investigated the in vivo metabolism of [18F]UCB-H and confirmed the negligible amount of radiometabolites in the rat brain. Hence, the in vivo quantification of SV2A using [18F]UCB-H microPET seems a promising tool for the assessment of the synaptic density in the rat brain, and opens the way for longitudinal follow-up in neurodegenerative diseases rodents’ models.
Research center :
GIGA CRC (Cyclotron Research Center) In vivo Imaging-Aging & Memory - ULiège
Disciplines :
Radiology, nuclear medicine & imaging
Author, co-author :
Becker, Guillaume ;  Université de Liège > Centre de recherches du cyclotron
Warnier, Corentin
Serrano Navacerrada, Maria Elisa ;  Université de Liège > Centre de recherches du cyclotron
Bahri, Mohamed Ali  ;  Université de Liège > Département de physique > Département de physique
Mercier, Joël
Lemaire, Christian ;  Université de Liège > Centre de recherches du cyclotron
Salmon, Eric  ;  Université de Liège > Département des sciences cliniques > Neuroimagerie des troubles de la mémoire et révalid. cogn.
Luxen, André ;  Université de Liège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse
Plenevaux, Alain  ;  Université de Liège > Département de chimie (sciences) > Département de chimie (sciences)
Language :
English
Title :
Pharmacokinetic characterization of [18F]UCB-H PET radiopharmaceutical in the rat brain.
Publication date :
26 June 2017
Journal title :
Molecular Pharmaceutics
ISSN :
1543-8384
eISSN :
1543-8392
Publisher :
American Chemical Society, Washington, United States - District of Columbia
Volume :
14
Issue :
8
Pages :
2719-2725
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Available on ORBi :
since 27 June 2017

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