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Radiosynthesis and first small animal microPET imaging of [18F]UCB-H, a new fluorine-18 labelled tracer targeting synaptic vesicle protein 2A (SV2A)
Aerts, Joël; Otabashi, Muhamed; Giacomelli, Fabrice et al.
201326th Annual Congress of the EANM
 

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Keywords :
PET; 18F; SV2A; Epilepsy
Abstract :
[en] Aim. We report the radiosynthesis and first rat microPET imaging of a new fluorine-18 tracer targeting the synaptic vesicle protein 2A, SV2A, identified as the binding site of the antiepileptic drug levetiracetam. Materials and Method. Two different nucleophilic radiosynthesis pathways were tested to obtain [18F]UCB-H, a no-carrier-added tracer in the 2-[18F]fluoropyridine family. The methods were automated on FastLab™ synthesizers. PET studies in rodents were carried out using male SD rats, imaged under isoflurane anaesthesia in a Siemens Concorde Focus 120 microPET scanner. Arterial input function was measured using an arteriovenous shunt method and beta microprobe system. All animal protocols were reviewed and accepted by animal ethical committees. Results and conclusion. A radiosynthesis yield of 30% was obtained (uncorrected for decay, 150 minutes of synthesis). Analytical methods were developed and validated to demonstrate that the quality of the tracer solution was compatible with in vivo injection. After intravenous injection, the tracer rapidly entered the brain, followed by rapid washout. PET imaging revealed high uptake of the tracer in the brain and spinal cord, matching the expected SV2A homogeneous distribution. Results indicate that [18F]UCB-H is suitable to quantify SV2A proteins in vivo and to estimate target occupancy of drugs targeting SV2A. Acknowledgments. The authors thank UCB Pharma SA Belgium for collaboration and the Walloon Region Belgium and the FRNS Belgium for financial support.
Disciplines :
Radiology, nuclear medicine & imaging
Author, co-author :
Aerts, Joël ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Otabashi, Muhamed;  Université de Liège - ULiège
Giacomelli, Fabrice ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Warnock, Geoffrey;  Université de Liège - ULiège > Centre de recherches du cyclotron
Bahri, Mohamed Ali  ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Bretin, Florian ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Sauvage, Xavier;  Université de Liège - ULiège > Centre de recherches du cyclotron
Thielen, Caroline ;  Université de Liège - ULiège > GIGA - Neurosciences
Lemaire, Christian ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Salmon, Eric  ;  Université de Liège - ULiège > Département des sciences cliniques > Neuroimagerie des troubles de la mémoire et révalid. cogn.
Plenevaux, Alain  ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Luxen, André ;  Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse
Language :
English
Title :
Radiosynthesis and first small animal microPET imaging of [18F]UCB-H, a new fluorine-18 labelled tracer targeting synaptic vesicle protein 2A (SV2A)
Alternative titles :
[en] A. Plenevaux, A. Luxen;
Publication date :
2013
Event name :
26th Annual Congress of the EANM
Event date :
du 19 octobre 2013 au 23 octobre 2013
References of the abstract :
European Journal of Nuclear Medicine and Molecular Imaging October 2013, Volume 40, Issue 2 Supplement, pp 89-565 EANM Abstracts 2013, OP680
Available on ORBi :
since 06 March 2014

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