UCB-J is a positron emission tomograp (PET) radioligand for the synaptic vesicle protein 2A (SV2A)[1][2][3][4].
UCB-J exhibits high free fraction (0.46 ± 0.02) and metabolizes at a moderate rate (39% ± 5% and 24% ± 3% parent remaining at 30 and 90 min) in plasma[3].
UCB-J displays high uptake and fast kinetics in the monkey brain[3].
When the animal is pretreated with UCB-J (150 μg/kg, iv), the whole brain SUV decreases to the same level as centrum semiovale, indicating the in vivo binding specificity of [18F]7 to SV2A[4].
[1]. JoËl Mercier, et al. Discovery of heterocyclic nonacetamide synaptic vesicle protein 2A (SV2A) ligands with single-digit nanomolar potency: opening avenues towards the first SV2A positron emission tomograp (PET) ligands. ChemMedChem. 2014 Apr;9(4):693-8.
[2]. Aline Delva, et al. Loss of Presynaptic Terminal Integrity in the Substantia Nigra in Early Parkinson's Disease. Mov Disord. 2020 Aug 7.
[3]. Nabeel B Nabulsi, et al. Synthesis and Preclinical Evaluation of 11C-UCB-J as a PET Tracer for Imaging the Synaptic Vesicle Glycoprotein 2A in the Brain. J Nucl Med. 2016 May;57(5):777-84.
[4]. Zhengxin Cai, et al. Synthesis and Preclinical Evaluation of an 18 F-Labeled Synaptic Vesicle Glycoprotein 2A PET Imaging Probe: [ 18 F]SynVesT-2. ACS Chem Neurosci. 2020 Feb 19;11(4):592-603.