ArticleNuclear medicine and biology2013
[18F]FMeNER-D2: reliable fully-automated synthesis for visualization of the norepinephrine transporter.
Article in Nuclear medicine and biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Sulfur [Journal of the American Chemical Society · 2021Article
- Association of norepinephrine transporter methylation with in vivo NET expression and hyperactivity-impulsivity symptoms in ADHD measured with PET.Molecular psychiatry · 2021Article
- Recent advances in radiotracers targeting norepinephrine transporter: structural development and radiolabeling improvements.Journal of neural transmission (Vienna, Austria : 1996) · 2020Review
- Effects of norepinephrine transporter gene variants on NET binding in ADHD and healthy controls investigated by PET.Human brain mapping · 2016Article
- Radiosynthesis and first preclinical evaluation of the novel norepinephrine transporter pet-ligand [(11)C]ME@HAPTHI.EJNMMI research · 2015Article
- Methods to Increase the Metabolic Stability of (18)F-Radiotracers.Molecules (Basel, Switzerland) · 2015Review
- The norepinephrine transporter in attention-deficit/hyperactivity disorder investigated with positron emission tomography.JAMA psychiatry · 2014Article
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Authors and funding
6 authors.
Funding
Abstract
purposeIn neurodegenerative diseases and neuropsychiatric disorders dysregulation of the norepinephrine transporter (NET) has been reported. For visualization of NET availability and occupancy in the human brain PET imaging can be used. Therefore, selective NET-PET tracers with high affinity are required. Amongst these, [(18)F]FMeNER-D2 is showing the best results so far. Furthermore, a reliable fully automated radiosynthesis is a prerequisite for successful application of PET-tracers. The aim of this work was the automation of [(18)F]FMeNER-D2 radiolabelling for subsequent clinical use. The presented study comprises 25 automated large-scale syntheses, which were directly applied to healthy volunteers and adult patients suffering from attention deficit hyperactivity disorder (ADHD). PROCEDURES: Synthesis of [(18)F]FMeNER-D2 was automated within a Nuclear Interface Module. Starting from 20-30 GBq [(18)F]fluoride, azeotropic drying, reaction with Br2CD2, distillation of 1-bromo-2-[(18)F]fluoromethane-D2 ([(18)F]BFM) and reaction of the pure [(18)F]BFM with unprotected precursor NER were optimized and completely automated. HPLC purification and SPE procedure were completed, formulation and sterile filtration were achieved on-line and full quality control was performed.
resultsPurified product was obtained in a fully automated synthesis in clinical scale allowing maximum radiation safety and routine production under GMP-like manner. So far, more than 25 fully automated syntheses were successfully performed, yielding 1.0-2.5 GBq of formulated [(18)F]FMeNER-D2 with specific activities between 430 and 1707 GBq/μmol within 95 min total preparation time.
conclusionsA first fully automated [(18)F]FMeNER-D2 synthesis was established, allowing routine production of this NET-PET tracer under maximum radiation safety and standardization.
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