ArticleJournal of medicinal chemistry2009
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
8 citing papers in PubMed, 33 citations in OpenAlex.
- Compartmental modeling of [(11)C]MENET binding to the norepinephrine transporter in the healthy human brain.Nuclear medicine and biology · 2016Trial
- Focus on Human Monoamine Transporter Selectivity. New Human DAT and NET Models, Experimental Validation, and SERT Affinity Exploration.ACS chemical neuroscience · 2020Article
- PET Radiotracers for CNS-Adrenergic Receptors: Developments and Perspectives.Molecules (Basel, Switzerland) · 2020Review
- Article
- Small Molecule Radiopharmaceuticals - A Review of Current Approaches.Frontiers in medicine · 2016Review
- Radiosynthesis and first preclinical evaluation of the novel norepinephrine transporter pet-ligand [(11)C]ME@HAPTHI.EJNMMI research · 2015Article
- (R)-N-Methyl-3-(3'-[F]fluoropropyl)phenoxy)-3-phenylpropanamine (F-MFP3) as a potential PET imaging agent for norepinephrine transporter.Journal of labelled compounds & radiopharmaceuticals · 2010Article
- Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine.PET clinics · 2009Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
Reboxetine analogues with methyl and fluoroalkyl substituents at position 2 of the phenoxy ring 1-4 were synthesized. In vitro competition binding with [(3)H]nisoxetine demonstrated that 1-4 have a high affinity for the norepinephrine transporter (NET) with K(i)'s = 1.02, 3.14, 3.68, and 0.30 nM, respectively. MicroPET imaging in rhesus monkeys showed that the relative regional distribution of [(11)C]1 and [(11)C]4 is consistent with distribution of the NET in the brain, while [(18)F]2 and [(18)F]3 showed only slight regional differentiation in brain uptake. Especially, the highest ratios of uptake of [(11)C]1 in NET-rich regions to that in caudate were obtained at 1.30-1.45 at 45 min and remained relatively constant over 85 min. Pretreatment of the monkey with the selective NET inhibitor, desipramine, decreased the specific binding for both [(11)C]1 and [(11)C]4. PET imaging in awake monkeys suggested that anesthesia influenced the binding potential of [(11)C]1 and [(11)C]4 at the NET.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.