ArticleJournal of medicinal chemistry2013
Derivatives of dibenzothiophene for positron emission tomography imaging of α7-nicotinic acetylcholine receptors.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers, 1 of them a synthesis that pooled it.
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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
29 citing papers in PubMed, 1 synthesis or guideline pooled it.
- 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
- Assessment of [Biomolecules · 2025Article
- Advances in PET Imaging of α7 Nicotinic Receptors: From Radioligand Development to CNS Applications.Basic & clinical pharmacology & toxicology · 2025Review
- Article
- Synthesis and Evaluation of Compound Targeting α7 and β2 Subunits in Nicotinic Acetylcholinergic Receptor.Molecules (Basel, Switzerland) · 2023Article
- Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography.Journal of medicinal chemistry · 2023Review
- Nicotinic Acetylcholine Receptors and Microglia as Therapeutic and Imaging Targets in Alzheimer's Disease.Molecules (Basel, Switzerland) · 2022Review
- PET Imaging in Animal Models of Alzheimer's Disease.Frontiers in neuroscience · 2022Review
- Positron Emission Tomography in Animal Models of Alzheimer's Disease Amyloidosis: Translational Implications.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Article
- Prodromal neuroinflammatory, cholinergic and metabolite dysfunction detected by PET and MRS in the TgF344-AD transgenic rat model of AD: a collaborative multi-modal study.Theranostics · 2021Article
- Article
- The Availability of the α7-Nicotinic Acetylcholine Receptor in Early Identification of Vulnerable Atherosclerotic Plaques: A Study Using a NovelFrontiers in bioengineering and biotechnology · 2021Article
- Use of 55 PET radiotracers under approval of a Radioactive Drug Research Committee (RDRC).EJNMMI radiopharmacy and chemistry · 2020Article
- Longitudinal PET Imaging of α7 Nicotinic Acetylcholine Receptors with [Molecular imaging and biology · 2020Article
- In Vitro and In Vivo Characterization of Dibenzothiophene Derivatives [Molecules (Basel, Switzerland) · 2020Article
- Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development.European journal of nuclear medicine and molecular imaging · 2020Review
- Radioiodinated 9-fluorenone derivatives for imaging α7-nicotinic acetylcholine receptors.MedChemComm · 2019Article
- Opportunities in precision psychiatry using PET neuroimaging in psychosis.Neurobiology of disease · 2019Review
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
A new series of derivatives of 3-(1,4-diazabicyclo[3.2.2]nonan-4-yl)dibenzo[b,d]thiophene 5,5-dioxide with high binding affinities and selectivity for α7-nicotinic acetylcholine receptors (α7-nAChRs) (Ki = 0.4-20 nM) has been synthesized for positron emission tomography (PET) imaging of α7-nAChRs. Two radiolabeled members of the series [(18)F]7a (Ki = 0.4 nM) and [(18)F]7c (Ki = 1.3 nM) were synthesized. [(18)F]7a and [(18)F]7c readily entered the mouse brain and specifically labeled α7-nAChRs. The α7-nAChR selective ligand 1 (SSR180711) blocked the binding of [(18)F]7a in the mouse brain in a dose-dependent manner. The mouse blocking studies with non-α7-nAChR central nervous system drugs demonstrated that [(18)F]7a is highly α7-nAChR selective. In agreement with its binding affinity the binding potential of [(18)F]7a (BPND = 5.3-8.0) in control mice is superior to previous α7-nAChR PET radioligands. Thus, [(18)F]7a displays excellent imaging properties in mice and has been chosen for further evaluation as a potential PET radioligand for imaging of α7-nAChR in non-human primates.
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Registered trials
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