Trial reportJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism2014
Determination of [(11)C]PBR28 binding potential in vivo: a first human TSPO blocking study.
Trial report in Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 79 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
79 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Positron Emission Tomography Studies of the Glial Cell Marker Translocator Protein in Patients With Psychosis: A Meta-analysis Using Individual Participant Data.Biological psychiatry · 2018Pooled it
- Confirmation of Specific Binding of the 18-kDa Translocator Protein (TSPO) Radioligand [Molecular imaging and biology · 2019Trial
- Building a database for brain 18 kDa translocator protein imaged using [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2019Trial
- Kinetic modelling of [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2018Trial
- Minocycline reduces chronic microglial activation after brain trauma but increases neurodegeneration.Brain : a journal of neurology · 2018Trial
- The PET Radioligand 18F-FIMX Images and Quantifies Metabotropic Glutamate Receptor 1 in Proportion to the Regional Density of Its Gene Transcript in Human Brain.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2016Trial
- Test-retest reproducibility of [(11)C]PBR28 binding to TSPO in healthy control subjects.European journal of nuclear medicine and molecular imaging · 2016Trial
- Cerebellum Can Serve As a Pseudo-Reference Region in Alzheimer Disease to Detect Neuroinflammation Measured with PET Radioligand Binding to Translocator Protein.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2015Trial
- Preliminary evidence of neuroimmune system disruption in opioid use disorder: Findings from a pilot PET TSPO imaging study.Brain, behavior, & immunity - health · 2026Article
- Alleviation of mutant TDP-43-mediated neuropathology by inducible stem cells in monkeys.International journal of biological sciences · 2026Article
- Exploratory study of peripheral immune changes associated with diffusion MRI multi-compartment model in temporal lobe epilepsy.Epilepsia · 2025Article
- TSPO circadian pattern: a test-retest study of [European journal of nuclear medicine and molecular imaging · 2025Article
- Evidence for brain glial activity in chronic migraine patients: a [European journal of nuclear medicine and molecular imaging · 2025Article
- A New Approach to Synthesize Carbon-11-PBR28 and its Clinical Validation in ALS Patients.Current radiopharmaceuticals · 2025Article
- Microglia-mediated neuroimmune suppression in PTSD is associated with anhedonia.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Misfolded protein deposits in Parkinson's disease and Parkinson's disease-related cognitive impairment, a [NPJ Parkinson's disease · 2024Article
- Differences in neuroinflammation in people who started antiretroviral treatment during primary versus chronic HIV infection: an 18kDa Translocator protein (TSPO) positron emission tomography (PET) study.Journal of neurovirology · 2024Observational
- [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2024Article
- Microglial Positron Emission Tomography Imaging In Vivo : Positron Emission Tomography Radioligands: Utility in Research and Clinical Practice.Advances in neurobiology · 2024Review
- Increased microglia activation in late non-central nervous system cancer survivors links to chronic systemic symptomatology.Human brain mapping · 2023Article
19 more citing papers are in PubMed but not listed here.
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Authors and funding
16 authors.
Funding
Abstract
Positron emission tomography (PET) targeting the 18 kDa translocator protein (TSPO) is used to quantify neuroinflammation. Translocator protein is expressed throughout the brain, and therefore a classical reference region approach cannot be used to estimate binding potential (BPND). Here, we used blockade of the TSPO radioligand [(11)C]PBR28 with the TSPO ligand XBD173, to determine the non-displaceable volume of distribution (VND), and hence estimate the BPND. A total of 26 healthy volunteers, 16 high-affinity binders (HABs) and 10 mixed affinity binders (MABs) underwent a [(11)C]PBR28 PET scan with arterial sampling. Six of the HABs received oral XBD173 (10 to 90 mg), 2 hours before a repeat scan. In XBD173-dosed subjects, VND was estimated via the occupancy plot. Values of BPND for all subjects were calculated using this VND estimate. Total volume of distribution (VT) of MABs (2.94±0.31) was lower than VT of HABs (4.33±0.29) (P<0.005). There was dose-dependent occupancy of TSPO by XBD173 (ED50=0.34±0.13 mg/kg). The occupancy plot provided a VND estimate of 1.98 (1.69, 2.26). Based on these VND estimates, BPND for HABs is approximately twice that of MABs, consistent with predictions from in vitro data. Our estimates of [(11)C]PBR28 VND and hence BPND in the healthy human brain are consistent with in vitro predictions. XBD173 blockade provides a practical means of estimating VND for TSPO targeting radioligands.
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