ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2015
Test-retest reproducibility of binding parameters in humans with 11C-LY2795050, an antagonist PET radiotracer for the κ opioid receptor.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 39 citations in OpenAlex.
- Recent advances in [Nuclear medicine and biology · 2026Review
- Kappa opioid receptor antagonism in neuropsychiatry: from molecular mechanisms to clinical prospects.European archives of psychiatry and clinical neuroscience · 2026Review
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- Strategies for the Production of [Organic process research & development · 2023Article
- The opioid system in depression.Neuroscience and biobehavioral reviews · 2022Review
- Low-Dose Augmentation With Buprenorphine for Treatment-Resistant Depression: A Multisite Randomized Controlled Trial With Multimodal Assessment of Target Engagement.Biological psychiatry global open science · 2022Article
- Evaluation of Specific Binding of [ACS medicinal chemistry letters · 2021Article
- First-in-Human Assessment ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Article
- The molecular neurobiology and neuropathology of opioid use disorder.Current research in neurobiology · 2021Article
- Rapid-Onset Anti-Stress Effects of a Kappa-Opioid Receptor Antagonist, LY2795050, Against Immobility in an Open Space Swim Paradigm in Male and Female Mice.Frontiers in pharmacology · 2021Article
- Use of 55 PET radiotracers under approval of a Radioactive Drug Research Committee (RDRC).EJNMMI radiopharmacy and chemistry · 2020Article
- Kinetic Modeling and Test-Retest Reproducibility ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- Synthesis and Pharmacological Evaluation of Fluorinated Quinoxaline-Based κ-Opioid Receptor (KOR) Agonists Designed for PET Studies.ChemMedChem · 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
- A Survey of Molecular Imaging of Opioid Receptors.Molecules (Basel, Switzerland) · 2019Review
- Impact of Pharmacological Manipulation of theThe Journal of pharmacology and experimental therapeutics · 2019Article
- Endogenous opioid system dysregulation in depression: implications for new therapeutic approaches.Molecular psychiatry · 2019Review
- Molecular Imaging of Opioid and Dopamine Systems: Insights Into the Pharmacogenetics of Opioid Use Disorders.Frontiers in psychiatry · 2019Review
- Radiosynthesis of [ACS medicinal chemistry letters · 2018Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
Abstract
unlabelled(11)C-LY2795050 is a new antagonist PET radioligand for the κ opioid receptor (KOR). In this study, we assessed the reproducibility of the binding parameters of (11)C-LY2795050 in healthy human subjects.
methodsSixteen healthy subjects (11 men and 5 women) underwent 2 separate 90-min PET scans with arterial input function and plasma free fraction (fP) measurements. The 2-tissue-compartment model and multilinear analysis-1 were applied to calculate 5 outcome measures in 14 brain regions: distribution volume (VT), VT normalized by fP (VT/fP), and 3 binding potentials (nondisplaceable binding potential, binding potential relative to total plasma concentration, and binding potential relative to free plasma concentration: BPND, BPP, BPF, respectively). Since KOR is distributed ubiquitously throughout the brain, there are no suitable reference regions. We used a fixed fraction of individual cerebellar VT value (VT,CER) as the nondisplaceable VT (VND) (VND = VT,CER/1.17). The relative and absolute test-retest variability and intraclass correlation coefficient were evaluated for the outcome measures of (11)C-LY2795050.
resultsThe test-retest variability of (11)C-LY2795050 for VT was no more than 10% in any region and was 12% in the amygdala. For binding potential (BPND and BPP), the test-retest variability was good in regions of moderate and high KOR density (BPND > 0.4) and poor in regions of low density. Correction by fP (VT/fP or BPF) did not improve the test-retest performance.
conclusionOur results suggest that quantification of (11)C-LY2795050 imaging is reproducible and reliable in regions with moderate and high KOR density. Therefore, we conclude that this first antagonist radiotracer is highly useful for PET studies of KOR.
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