Abstract
An automated radiosynthesis of carbon‐11 positron emission tomography radiotracer [11C]UCB‐J for imaging the synaptic density biomarker synaptic vesicle glycoprotein SV2A was established using Synthra RNPlus synthesizer. Commercially available trifluoroborate UCB‐J analogue was used as a radiolabelling precursor, and the desired radiolabelled product was isolated in 11 ± 2% (n = 7) nondecay corrected radiochemical yield and formulated as a 10% EtOH solution in saline with molar activities of 20 to 100 GBq/μmol. The method was based upon the palladium(0)‐mediated Suzuki cross‐coupling reaction and [11C]CH3I as a radiolabelling synthon. The isolated product was cGMP compliant as demonstrated by the results of quality control analysis.
Highlights
Developed is a noninvasive alternative using positron emission tomography (PET), which for the first time enables the quantification of synaptic density in vivo
Further investigation indicated that while trifluoroborate 3 can be used as a radiolabelling precursor for [11C]UCB-J, the actual reacting specie is the boronic acid, necessitating a need for a mixture of trifluoroborate 3 and 3-10% of the boronic acid 4 to be present in the reaction vessel.[11,14]
Reproducible radiosynthesis of [11C]UCB-J using the Synthra RNPlus automated synthesizer has been achieved with RCY at end of synthesis comparable to that reported and in compliance with the cGMP regulations
Summary
Involved in processes of higher brain functions such as information processing (eg, thinking) or changes. Developed is a noninvasive alternative using positron emission tomography (PET), which for the first time enables the quantification of synaptic density in vivo. This is achieved by radiotracers selective to synaptic vesicle glycoprotein SV2A, a transmembrane protein expressed ubiquitously in secretory vesicles in all brain areas.[8] Arising from several structural scaffolds related to the antiepileptic drug levetiracetam (LEV, 1; Figure 1)[9] the carbon-11 radiolabelled UCB-J analogue ([11C]2; Figure 1) has been shown to have excellent in vitro and in vivo properties for imaging SV2A from both preclinical and clinical studies.[7,10]. To undertake clinical SV2A PET studies at our centre, our objective was to establish a manufacturing method for [11C]UCB-J for which a radiosynthesis method has been developed.[7,10,11] we report development of the fully automated and cGMP compliant radiosynthesis of [11C]UCB-J using Synthra RNPlus automated radiosynthesizer
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