RT Journal Article SR Electronic T1 Evaluation of 18F-UCB-H as a Novel PET Tracer for Synaptic Vesicle Protein 2A in the Brain JF Journal of Nuclear Medicine JO J Nucl Med FD Society of Nuclear Medicine SP 1336 OP 1341 DO 10.2967/jnumed.113.136143 VO 55 IS 8 A1 Geoffrey I. Warnock A1 Joël Aerts A1 Mohamed Ali Bahri A1 Florian Bretin A1 Christian Lemaire A1 Fabrice Giacomelli A1 Frederic Mievis A1 Nathalie Mestdagh A1 Tim Buchanan A1 Anne Valade A1 Joël Mercier A1 Martyn Wood A1 Michel Gillard A1 Alain Seret A1 André Luxen A1 Eric Salmon A1 Alain Plenevaux YR 2014 UL http://jnm.snmjournals.org/content/55/8/1336.abstract AB Synaptic vesicle protein 2 isoforms are critical for proper nervous system function and are involved in vesicle trafficking. The synaptic vesicle protein 2A (SV2A) isoform has been identified as the binding site of the antiepileptic levetiracetam (LEV), making it an interesting therapeutic target for epilepsy. 18F-UCB-H is a novel PET imaging agent with a nanomolar affinity for human SV2A. Methods: Preclinical PET studies were performed with isoflurane-anesthetized rats. The arterial input function was measured with an arteriovenous shunt and a β-microprobe system. 18F-UCB-H was injected intravenously (bolus of 140 ± 20 MBq). Results: Brain uptake of 18F-UCB-H was high, matching the expected homogeneous distribution of SV2A. The distribution volume (Vt) for 18F-UCB-H was calculated with Logan graphic analysis, and the effect of LEV pretreatment on Vt was measured. In control animals the whole-brain Vt was 9.76 ± 0.52 mL/cm3 (mean ± SD; n = 4; test–retest), and the reproducibility in test–retest studies was 10.4% ± 6.5% (mean ± SD). The uptake of 18F-UCB-H was dose dependently blocked by pretreatment with LEV (0.1–100 mg/kg intravenously). Conclusion: Our results indicated that 18F-UCB-H is a suitable radiotracer for the imaging of SV2A in vivo. To our knowledge, this is the first PET tracer for the in vivo quantification of SV2A. The necessary steps for the implementation of 18F-UCB-H production under good manufacturing practice conditions and the first human studies are being planned.