ArticleNeurobiology of disease2008
The high affinity peripheral benzodiazepine receptor ligand DAA1106 binds to activated and infected brain macrophages in areas of synaptic degeneration: implications for PET imaging of neuroinflammation in lentiviral encephalitis.
Article in Neurobiology of disease, 2008. 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, 26 citations in OpenAlex.
- 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
- 18 kDa TSPO targeting drives polarized human microglia towards a protective and restorative neurosteroidome profile.Cellular and molecular life sciences : CMLS · 2025Article
- The translocator protein ligands as mitochondrial functional modulators for the potential anti-Alzheimer agents.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Positron Emission Tomography Techniques to Measure Active Inflammation, Fibrosis and Angiogenesis: Potential for Non-invasive Imaging of Hypertensive Heart Failure.Frontiers in cardiovascular medicine · 2021Review
- [European journal of nuclear medicine and molecular imaging · 2020Article
- Concentration, distribution, and influence of aging on the 18 kDa translocator protein in human brain: Implications for brain imaging studies.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2020Article
- Lack of neuroinflammation in the HIV-1 transgenic rat: an [(18)F]-DPA714 PET imaging study.Journal of neuroinflammation · 2015Article
- Review
- Noninvasive molecular imaging of neuroinflammation.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2012Review
- Current imaging strategies in rheumatoid arthritis.American journal of nuclear medicine and molecular imaging · 2012Article
- Evaluation of translocator protein quantification as a tool for characterising macrophage burden in human carotid atherosclerosis.Atherosclerosis · 2010Article
- Cyclooxygenase and neuroinflammation in Parkinson's disease neurodegeneration.Current neuropharmacology · 2010Article
- Expression of the translocator protein of 18 kDa by microglia, macrophages and astrocytes based on immunohistochemical localization in abnormal human brain.Neuropathology and applied neurobiology · 2009Article
- Imaging microglial activation during neuroinflammation and Alzheimer's disease.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2009Review
- Carbon 11-labeled Pittsburgh Compound B and carbon 11-labeled (R)-PK11195 positron emission tomographic imaging in Alzheimer disease.Archives of neurology · 2009Article
- The positron emission tomography ligand DAA1106 binds with high affinity to activated microglia in human neurological disorders.Journal of neuropathology and experimental neurology · 2008Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
HIV encephalitis (HIVE) is characterized by neurodegeneration mediated by toxins derived from infected and activated brain macrophages. Since the peripheral benzodiazepine receptor (PBR) is abundant on brain macrophages, we hypothesized that [(3)H]DAA1106, a new PBR ligand, can label infected and activated brain macrophages in HIVE. Using cell culture and postmortem brain tissues from HIVE and a macaque model of HIVE, we show that [(3)H]DAA1106 binds with high affinity to activated and infected macrophages in regions of synaptic damage. Further, binding affinity reflected by lower K(D) (dissociation constant) values and the B(max) (total number of binding sites) to K(D) ratios reflective of ligand-binding potential was significantly higher with [(3)H]DAA1106 compared to the extensively characterized PBR ligand [(3)H](R)-PK11195. These data suggest that DAA1106 binds with high affinity to activated and infected brain macrophages and possesses binding characteristics beneficial for in vivo use in the detection and clinical monitoring of HIVE using positron emission tomography.
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