ArticleEuropean journal of nuclear medicine and molecular imaging2011
Assessment of α7 nicotinic acetylcholine receptor availability in juvenile pig brain with [¹⁸F]NS10743.
Article in European journal of nuclear medicine and molecular imaging, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Human brain imaging of α7 nAChR with [(18)F]ASEM: a new PET radiotracer for neuropsychiatry and determination of drug occupancy.Molecular imaging and biology · 2014Trial
- Advances in PET Imaging of α7 Nicotinic Receptors: From Radioligand Development to CNS Applications.Basic & clinical pharmacology & toxicology · 2025Review
- Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography.Journal of medicinal chemistry · 2023Review
- The role of astrocytic α7 nicotinic acetylcholine receptors in Alzheimer disease.Nature reviews. Neurology · 2023Review
- In Vitro and In Vivo Characterization of Dibenzothiophene Derivatives [Molecules (Basel, Switzerland) · 2020Article
- Current radiotracers to image neurodegenerative diseases.EJNMMI radiopharmacy and chemistry · 2019Review
- PET imaging of αEuropean journal of nuclear medicine and molecular imaging · 2017Article
- Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.Current topics in medicinal chemistry · 2016Review
- Development of [(18)F]ASEM, a specific radiotracer for quantification of the α7-nAChR with positron-emission tomography.Biochemical pharmacology · 2015Review
- A Promising PET Tracer for Imaging of α₇ Nicotinic Acetylcholine Receptors in the Brain: Design, Synthesis, and in Vivo Evaluation of a Dibenzothiophene-Based Radioligand.Molecules (Basel, Switzerland) · 2015Article
- PET Imaging of the Human Nicotinic Cholinergic Pathway in Atherosclerosis.Current cardiology reports · 2015Review
- Development of (18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography.Neuroscience bulletin · 2014Review
- Imaging of α7 nicotinic acetylcholine receptors in brain and cerebral vasculature of juvenile pigs with [(18)F]NS14490.EJNMMI research · 2014Article
- Derivatives of dibenzothiophene for positron emission tomography imaging of α7-nicotinic acetylcholine receptors.Journal of medicinal chemistry · 2013Article
- Synthesis and evaluation of new radioligands [(11)C]A-833834 and [(11)C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors.Nuclear medicine and biology · 2013Article
- 5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole as a potential PET radioligand for imaging cerebral α7-nAChR in mice.Bioorganic & medicinal chemistry · 2012Article
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Authors and funding
10 authors.
Funding
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Abstract
purposeTo conduct a quantitative PET assessment of the specific binding sites in the brain of juvenile pigs for [(18)F]NS10743, a novel diazabicyclononane derivative targeting α7 nicotinic acetylcholine receptors (α7 nAChRs).
methodsDynamic PET recordings were made in isoflurane-anaesthetized juvenile pigs during 120 min after administration of [(18)F]NS10743 under baseline conditions (n = 3) and after blocking of the α7 nAChR with NS6740 (3 mg·kg(-1) bolus + 1 mg·kg(-1)·h(-1) continuous infusion; n = 3). Arterial plasma samples were collected for determining the input function of the unmetabolized tracer. Kinetic analysis of regional brain time-radioactivity curves was performed, and parametric maps were calculated relative to arterial input.
resultsPlasma [(18)F]NS10743 passed readily into the brain, with peak uptake occurring in α7 nAChR-expressing brain regions such as the colliculi, thalamus, temporal lobe and hippocampus. The highest SUV(max) was approximately 2.3, whereas the lowest uptake was in the olfactory bulb (SUV(max) 1.53 ± 0.32). Administration of NS6740 significantly decreased [(18)F]NS10743 binding late in the emission recording throughout the brain, except in the olfactory bulb, which was therefore chosen as reference region for calculation of BP(ND). The baseline BP(ND) ranged from 0.39 ± 0.08 in the cerebellum to 0.76 ± 0.07 in the temporal lobe. Pretreatment and constant infusion with NS6740 significantly reduced the BP(ND) in regions with high [(18)F]NS10743 binding (temporal lobe -29%, p = 0.01; midbrain: -35%, p = 0.02), without significantly altering the BP(ND) in low binding regions (cerebellum: -16%, p = 0.2).
conclusionThis study confirms the potential of [(18)F]NS10743 as a target-specific radiotracer for the molecular imaging of central α7 nAChRs by PET.
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