ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2014
18F-ASEM, a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers, 1 of them a synthesis that pooled it.
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Who cites it
45 citing papers in PubMed, 1 synthesis or guideline pooled it, 77 citations in OpenAlex.
- Radiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade.International journal of molecular sciences · 2022Pooled it
- 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
- Curing the brain: in search for new astrocyte-specific therapies.Experimental & molecular medicine · 2026Review
- Assessment of [Biomolecules · 2025Article
- Article
- Neuronal and Glial α7 Nicotinic Acetylcholine Receptors: Role in Alzheimer's Disease Pathophysiology.Life (Basel, Switzerland) · 2025Review
- Advances in PET Imaging of α7 Nicotinic Receptors: From Radioligand Development to CNS Applications.Basic & clinical pharmacology & toxicology · 2025Review
- Evaluation of [Receptors (Basel, Switzerland) · 2025Article
- Advanced Imaging Techniques for Atherosclerosis and Cardiovascular Calcification in Animal Models.Journal of cardiovascular development and disease · 2024Review
- Hippocampal Availability of the α7 Nicotinic Acetylcholine Receptor in Recent-Onset Psychosis.JAMA network open · 2024Article
- Positron Emission Tomography Imaging of Synaptic Dysfunction in Parkinson's Disease.Neuroscience bulletin · 2024Review
- Synthesis and preclinical evaluation of [Scientific reports · 2024Article
- Article
- Characterizing the binding of TC-5619 and encenicline on the alpha7 nicotinic acetylcholine receptor using PET imaging in the pig.Frontiers in neuroimaging · 2024Article
- Synthesis and Evaluation of Compound Targeting α7 and β2 Subunits in Nicotinic Acetylcholinergic Receptor.Molecules (Basel, Switzerland) · 2023Article
- Multimodal Imaging for Validation and Optimization of Ion Channel-Based Chemogenetics in Nonhuman Primates.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2023Article
- 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
- Development ofACS chemical neuroscience · 2022Article
- Relative Strengths of Three Linearizations of Receptor Availability: Saturation, Inhibition, and Occupancy Plots.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
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Authors and funding
15 authors at 3 institutions in 1 country.
Funding
Abstract
unlabelledThe α7-nicotinic cholinergic receptor (α7-nAChR) is a key mediator of brain communication and has been implicated in a wide variety of central nervous system disorders. None of the currently available PET radioligands for α7-nAChR are suitable for quantitative PET imaging, mostly because of insufficient specific binding. The goal of this study was to evaluate the potential of (18)F-ASEM ((18)F-JHU82132) as an α7-nAChR radioligand for PET.
methodsThe inhibition binding assay and receptor functional properties of ASEM were assessed in vitro. The brain regional distribution of (18)F-ASEM in baseline and blockade were evaluated in DISC1 mice (dissection) and baboons (PET).
resultsASEM is an antagonist for the α7-nAChR with high binding affinity (Ki = 0.3 nM). (18)F-ASEM readily entered the baboon brain and specifically labeled α7-nAChR. The in vivo specific binding of (18)F-ASEM in the brain regions enriched with α7-nAChRs was 80%-90%. SSR180711, an α7-nAChR-selective partial agonist, blocked (18)F-ASEM binding in the baboon brain in a dose-dependent manner, suggesting that the binding of (18)F-ASEM was mediated by α7-nAChRs and the radioligand was suitable for drug evaluation studies. In the baboon baseline studies, the brain regional volume of distribution (VT) values for (18)F-ASEM were 23 (thalamus), 22 (insula), 18 (hippocampus), and 14 (cerebellum), whereas in the binding selectivity (blockade) scan, all regional VT values were reduced to less than 4. The range of regional binding potential values in the baboon brain was from 3.9 to 6.6. In vivo cerebral binding of (18)F-ASEM and α7-nAChR expression in mutant DISC1 mice, a rodent model of schizophrenia, was significantly lower than in control animals, which is in agreement with previous postmortem human data.
conclusion(18)F-ASEM holds promise as a radiotracer with suitable imaging properties for quantification of α7-nAChR in the human brain.
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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.