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Evaluating the In Vivo Specificity of [18F]UCB-H for the SV2A Protein, Compared with SV2B and SV2C in Rats Using microPET

1
GIGA—CRC In Vivo Imaging, University of Liège, 8 Allée du 6 Août, Building B30, Sart Tilman, 4000 Liège, Belgium
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UCB Pharma s.a., 1420 Braine-l’Alleud, Belgium
3
Nucleis s.a., University of Liège, 8 Allée du 6 Août, Building B30, Sart Tilman, 4000 Liège, Belgium
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(9), 1705; https://doi.org/10.3390/molecules24091705
Received: 22 March 2019 / Revised: 28 April 2019 / Accepted: 29 April 2019 / Published: 1 May 2019
(This article belongs to the Special Issue Radiolabelled Molecules for Brain Imaging with PET and SPECT)
The synaptic vesicle protein 2 (SV2) is involved in synaptic vesicle trafficking. The SV2A isoform is the most studied and its implication in epilepsy therapy led to the development of the first SV2A PET radiotracer [18F]UCB-H. The objective of this study was to evaluate in vivo, using microPET in rats, the specificity of [18F]UCB-H for SV2 isoform A in comparison with the other two isoforms (B and C) through a blocking assay. Twenty Sprague Dawley rats were pre-treated either with the vehicle, or with specific competitors against SV2A (levetiracetam), SV2B (UCB5203) and SV2C (UCB0949). The distribution volume (Vt, Logan plot, t* 15 min) was obtained with a population-based input function. The Vt analysis for the entire brain showed statistically significant differences between the levetiracetam group and the other groups (p < 0.001), but also between the vehicle and the SV2B group (p < 0.05). An in-depth Vt analysis conducted for eight relevant brain structures confirmed the statistically significant differences between the levetiracetam group and the other groups (p < 0.001) and highlighted the superior and the inferior colliculi along with the cortex as regions also displaying statistically significant differences between the vehicle and SV2B groups (p < 0.05). These results emphasize the in vivo specificity of [18F]UCB-H for SV2A against SV2B and SV2C, confirming that [18F]UCB-H is a suitable radiotracer for in vivo imaging of the SV2A proteins with PET. View Full-Text
Keywords: SV2A; SV2B; SV2C; microPET; [18F]UCB-H; epilepsy; PBIF; distribution volume; blocking assay; preclinical imaging SV2A; SV2B; SV2C; microPET; [18F]UCB-H; epilepsy; PBIF; distribution volume; blocking assay; preclinical imaging
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Serrano, M.E.; Becker, G.; Bahri, M.A.; Seret, A.; Mestdagh, N.; Mercier, J.; Mievis, F.; Giacomelli, F.; Lemaire, C.; Salmon, E.; Luxen, A.; Plenevaux, A. Evaluating the In Vivo Specificity of [18F]UCB-H for the SV2A Protein, Compared with SV2B and SV2C in Rats Using microPET. Molecules 2019, 24, 1705.

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