ArticleNuclear medicine and biology2015
Evaluation of [(18)F]-(-)-norchlorofluorohomoepibatidine ([(18)F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates.
Article in Nuclear medicine and biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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14 citing papers in PubMed, 18 citations in OpenAlex.
- Multiple sources of β2*-nicotinic acetylcholine receptor binding are differentially affected during tobacco smoking abstinence as revealed by Independent Component Analysis of [Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography.Journal of medicinal chemistry · 2023Review
- Cholinergic system adaptations are associated with cognitive function in people recently abstinent from smoking: a (-)-[Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- Intrahippocampal blockade of nicotinic or muscarinic receptors fails to impair nonnavigational spatial memory in macaques.Behavioral neuroscience · 2021Article
- PET Imaging Estimates of Regional Acetylcholine Concentration Variation in Living Human Brain.Cerebral cortex (New York, N.Y. : 1991) · 2021Article
- Dealing with PET radiometabolites.EJNMMI research · 2020Review
- Use of Electronic Cigarettes Leads to Significant Beta2-Nicotinic Acetylcholine Receptor Occupancy: Evidence From a PET Imaging Study.Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco · 2018Article
- Evaluation of (-)-[Synapse (New York, N.Y.) · 2018Article
- Exploring the Metabolism of (+)-[Molecules (Basel, Switzerland) · 2018Article
- Quinuclidine and DABCO Enhance the Radiofluorinations of 5-Substituted 2-Halopyridines.European journal of organic chemistry · 2017Article
- Imaging α4β2 Nicotinic Acetylcholine Receptors (nAChRs) in Baboons with [Molecular imaging and biology · 2017Article
- Automation of the Radiosynthesis of Six DifferentEJNMMI radiopharmacy and chemistry · 2017Article
- Article
- LC-MS Supported Studies on the in Vitro Metabolism of both Enantiomers of Flubatine and the in Vivo Metabolism of (+)-[(18)F]Flubatine-A Positron Emission Tomography Radioligand for Imaging α4β2 Nicotinic Acetylcholine Receptors.Molecules (Basel, Switzerland) · 2016Article
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8 authors at 1 institution in 1 country.
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Abstract
introductionThe aims of the present study were to develop an optimized microfluidic method for the production of the selective nicotinic acetylcholine α4β2 receptor radiotracer [(18)F]-(-)-NCFHEB ([(18)F]-Flubatine) and to investigate its receptor binding profile and pharmacokinetic properties in rhesus monkeys in vivo.
methods[(18)F]-(-)-NCFHEB was prepared in two steps, a nucleophilic fluorination followed by N-Boc deprotection. PET measurements were performed in rhesus monkeys including baseline and preblocking experiments with nicotine (0.24 mg/kg). Radiometabolites in plasma were measured using HPLC.
results[(18)F]-(-)-NCFHEB was prepared in a total synthesis time of 140 min. The radiochemical purity in its final formulation was >98% and the mean specific radioactivity was 97.3 ± 16.1 GBq/μmol (n = 6) at end of synthesis (EOS). In the monkey brain, radioactivity concentration was high in the thalamus, moderate in the putamen, hippocampus, frontal cortex, and lower in the cerebellum. Nicotine blocked 98-100% of [(18)F]-(-)-NCFHEB specific binding, and the non-displaceable distribution volume (VND) was estimated at 5.9 ± 1.0 mL/cm(3) (n = 2), or 6.6 ± 1.1 mL/cm(3) after normalization by the plasma free fraction fP. Imaging data are amenable to kinetic modeling analysis using the multilinear analysis (MA1) method, and model-derived binding parameters display good test-retest reproducibility. In rhesus monkeys, [(18)F]-(-)-NCFHEB can yield robust regional binding potential (BPND) values (thalamus = 4.1 ± 1.5, frontal cortex = 1.2 ± 0.2, putamen = 0.96 ± 0.45, and cerebellum = 0.10 ± 0.29).
conclusionAn efficient microfluidic synthetic method was developed for preparation of [(18)F]-(-)-NCFHEB. PET examination in rhesus monkeys showed that [(18)F]-(-)-NCFHEB entered the brain readily and its regional radioactivity uptake pattern was in accordance with the known distribution of α4β2 receptors. Estimated non-displaceable binding potential (BPND) values in brain regions were better than those of [(18)F]2-FA and comparable to [(18)F]AZAN. These results confirm previous findings and support further examination of [(18)F]-(-)-NCFHEB in humans.
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