ArticlePloS one2010
In vivo evaluation of alpha7 nicotinic acetylcholine receptor agonists [11C]A-582941 and [11C]A-844606 in mice and conscious monkeys.
Article in PloS one, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 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
- Good Manufacturing Practice Validation and Radiation Dosimetry for the Clinical Application of a Novel α7-nAChR Radioligand: [Molecules (Basel, Switzerland) · 2025Article
- Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography.Journal of medicinal chemistry · 2023Review
- Article
- Current radiotracers to image neurodegenerative diseases.EJNMMI radiopharmacy and chemistry · 2019Review
- 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
- Derivatives of dibenzothiophene for positron emission tomography imaging of α7-nicotinic acetylcholine receptors.Journal of medicinal chemistry · 2013Article
- The nicotinic acetylcholine receptor: smoking and Alzheimer's disease revisited.Frontiers in bioscience (Elite edition) · 2012Review
- Assessment of α7 nicotinic acetylcholine receptor availability in juvenile pig brain with [¹⁸F]NS10743.European journal of nuclear medicine and molecular imaging · 2011Article
- Functional promoter polymorphisms govern differential expression of HMG-CoA reductase gene in mouse models of essential hypertension.PloS one · 2011Article
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Authors and funding
7 authors.
Funding
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Abstract
backgroundThe alpha7 nicotinic acetylcholine receptors (nAChRs) play an important role in the pathophysiology of neuropsychiatric diseases such as schizophrenia and Alzheimer's disease. The goal of this study was to evaluate the two carbon-11-labeled alpha7 nAChR agonists [(11)C]A-582941 and [(11)C]A-844606 for their potential as novel positron emission tomography (PET) tracers. METHODOLOGY/PRINCIPAL
findingsThe two tracers were synthesized by methylation of the corresponding desmethyl precursors using [(11)C]methyl triflate. Effects of receptor blockade in mice were determined by coinjection of either tracer along with a carrier or an excess amount of a selective alpha7 nAChR agonist (SSR180711). Metabolic stability was investigated using radio-HPLC. Dynamic PET scans were performed in conscious monkeys with/without SSR180711-treatment. [(11)C]A-582941 and [(11)C]A-844606 showed high uptake in the mouse brain. Most radioactive compounds in the brain were detected as an unchanged form. However, regional selectivity and selective receptor blockade were not clearly observed for either compound in the mouse brain. On the other hand, the total distribution volume of [(11)C]A-582941 and [(11)C]A-844606 was high in the hippocampus and thalamus but low in the cerebellum in the conscious monkey brain, and reduced by pretreatment with SSR180711. CONCLUSIONS/SIGNIFICANCE: A nonhuman primate study suggests that [(11)C]A-582941 and [(11)C]A-844606 would be potential PET ligands for imaging alpha7 nAChRs in the human brain.
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