ArticleJournal of neuropathology and experimental neurology2008
The positron emission tomography ligand DAA1106 binds with high affinity to activated microglia in human neurological disorders.
Article in Journal of neuropathology and experimental neurology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT07233512 (EFFECT OF SURGICAL AND NON-SURGICAL PERIODONTAL TREATMENT ON ALZHEIMER DISEASE-ASSOCIATED OUTCOMES), which is not on this map. Cited by 71 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.
The trial behind it
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.
EFFECT OF SURGICAL AND NON-SURGICAL PERIODONTAL TREATMENT ON ALZHEIMER DISEASE-ASSOCIATED OUTCOMES: A Randomized Clinical Trial
Who cites it
71 citing papers in PubMed, 119 citations in OpenAlex.
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- Microglia modulate Aβ-dependent astrocyte reactivity in Alzheimer's disease.Nature neuroscience · 2026Article
- Exploring inflammation-related protein expression and its relationship with TSPO PET in Alzheimer's disease.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2025Article
- Cigarette smoking is associated with reduced neuroinflammation and better cognitive control in people living with HIV.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Effects of Cigarette Smoking and 3-Day Smoking Abstinence on Translocator Protein 18 kDa Availability: A [Addiction biology · 2025Observational
- Microglia in Health and Diseases: Integrative Hubs of the Central Nervous System (CNS).Cold Spring Harbor perspectives in biology · 2024Review
- The development status of PET radiotracers for evaluating neuroinflammation.Nuclear medicine and molecular imaging · 2024Review
- Astrocyte Regulation of Cerebral Blood Flow in Health and Disease.Cold Spring Harbor perspectives in biology · 2024Review
- Microglia measured by TSPO PET are associated with Alzheimer's disease pathology and mediate key steps in a disease progression model.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2024Article
- Microglial Positron Emission Tomography Imaging In Vivo : Positron Emission Tomography Radioligands: Utility in Research and Clinical Practice.Advances in neurobiology · 2024Review
- Microglial activation in the frontal cortex predicts cognitive decline in frontotemporal dementia.Brain : a journal of neurology · 2023Article
- Elevated GRO-α and IL-18 in serum and brain implicate the NLRP3 inflammasome in frontotemporal dementia.Scientific reports · 2023Article
- Article
- Molecular Imaging of Neuroinflammation in Alzheimer's Disease and Mild Cognitive Impairment.Advances in experimental medicine and biology · 2023Article
- The heterogeneity of microglial activation and its epigenetic and non-coding RNA regulations in the immunopathogenesis of neurodegenerative diseases.Cellular and molecular life sciences : CMLS · 2022Review
- Essential Principles and Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging.Current medicinal chemistry · 2022Review
- In vivo imaging translocator protein (TSPO) in autism spectrum disorder.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Novel brain PET imaging agents: Strategies for imaging neuroinflammation in Alzheimer's disease and mild cognitive impairment.Frontiers in immunology · 2022Review
- Microglia activation linking amyloid-β drive tau spatial propagation in Alzheimer's disease.Frontiers in neuroscience · 2022Article
- Frontotemporal dementia: A unique window on the functional role of the temporal lobes.Handbook of clinical neurology · 2022Review
11 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Chronic microglial activation is an important component of many neurological disorders, and imaging activated microglia in vivo will enable the detection and improved treatment of neuroinflammation. 1-(2-chlorphenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinoline-carbox-amide (PK11195), a peripheral benzodiazepine receptor ligand, has been used to image neuroinflammation, but the extent to which PK11195 binding distinguishes activated microglia and reactive astrocytes is unclear. Moreover, PK11195 may lack sufficient sensitivity for detecting mild neuroinflammation. We hypothesized that N-(2,5-dimethoxybenzyl)-N-(4-fluoro-2-phenoxyphenyl) acetamide (DAA1106), a new ligand that binds specifically to peripheral benzodiazepine receptor, binds to activated microglia in human neurological diseases with higher affinity than does PK11195. We therefore compared the pharmacological binding properties of [3H](R)-PK11195 and [3H]DAA1106 in postmortem tissues from patients with cerebral infarcts, amyotrophic lateral sclerosis, Alzheimer disease, frontotemporal dementia, and multiple sclerosis (n=10 each). In all diseases, [3H]DAA1106 showed a higher binding affinity as reflected by lower dissociation constant (KD) values than that of [3H](R)-PK11195. Moreover, specific binding of both ligands correlated with the presence of activated microglia identified by immunohistochemistry in situ. We conclude that 1) ligands that bind peripheral benzodiazepine receptor mainly label activated microglia in human neurological disorders and that 2) DAA1106 may possess binding characteristics superior to those of PK11195, which may be beneficial for in vivo positron emission tomography imaging.
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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.