Trial reportJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism2014
Kinetic modeling of (11)C-LY2795050, a novel antagonist radiotracer for PET imaging of the kappa opioid receptor in humans.
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 31 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
31 citing papers in PubMed, 48 citations in OpenAlex.
- Efficacy and safety of aticaprant, a kappa receptor antagonist, adjunctive to oral SSRI/SNRI antidepressant in major depressive disorder: results of a phase 2 randomized, double-blind, placebo-controlled study.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Trial
- Depression in neurodegenerative disease: neurobiological mechanisms and emerging treatments.Molecular psychiatry · 2026Review
- Recent advances in [Nuclear medicine and biology · 2026Review
- Kappa opioid receptor availability correlates with depressive symptom burden in chronic migraine: a preliminary investigation.The journal of headache and pain · 2026Article
- Automated Manufacturing of Carbon-11 Radiopharmaceuticals Using Cassette-Based Radiosynthesizers.Journal of labelled compounds & radiopharmaceuticals · 2025Review
- Copper-mediated radiochemistry: historical impact, current trends, and future possibilities.Npj imaging · 2025Review
- Numerical simulation method for the assessment of the effect of molar activity on the pharmacokinetics of radioligands in small animals.EJNMMI radiopharmacy and chemistry · 2024Article
- DOCK-PET: database of CNS kinetic parameters in the healthy human brain for existing PET tracers.Annals of nuclear medicine · 2024Article
- Development and Optimization ofACS pharmacology & translational science · 2023Review
- Strategies for the Production of [Organic process research & development · 2023Article
- Opioid antagonism in humans: a primer on optimal dose and timing for central mu-opioid receptor blockade.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- 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
- Brain opioid segments and striatal patterns of dopamine release induced by naloxone and morphine.Human brain mapping · 2022Article
- Imaging Kappa Opioid Receptors in the Living Brain with Positron Emission Tomography.Handbook of experimental pharmacology · 2022Review
- Evaluation of Specific Binding of [ACS medicinal chemistry letters · 2021Article
- Kinetic Modeling and Test-Retest Reproducibility ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 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
- Molecular Imaging of Opioid and Dopamine Systems: Insights Into the Pharmacogenetics of Opioid Use Disorders.Frontiers in psychiatry · 2019Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
12 authors at 3 institutions in 1 country.
Funding
Abstract
(11)C-LY2795050 is a novel kappa opioid receptor (KOR) antagonist tracer for positron emission tomography (PET) imaging. The purpose of this first-in-human study was to determine the optimal kinetic model for analysis of (11)C-LY2795050 imaging data. Sixteen subjects underwent baseline scans and blocking scans after oral naltrexone. Compartmental modeling and multilinear analysis-1 (MA1) were applied using the arterial input functions. Two-tissue compartment model and MA1 were found to be the best models to provide reliable measures of binding parameters. The rank order of (11)C-LY2795050 distribution volume (VT) matched the known regional KOR densities in the human brain. Blocking scans with naltrexone indicated no ideal reference region for (11)C-LY2795050. Three methods for calculation of the nondisplaceable distribution volume (VND) were assessed: (1) individual VND estimated from naltrexone occupancy plots, (2) mean VND across subjects, and (3) a fixed fraction of cerebellum VT. Approach (3) produced the lowest intersubject variability in the calculation of binding potentials (BPND, BPF, and BPP). Therefore, binding potentials of (11)C-LY2795050 can be determined if the specific binding fraction in the cerebellum is presumed to be unchanged by diseases and experimental conditions. In conclusion, results from the present study show the suitability of (11)C-LY2795050 to image and quantify KOR in humans.
Indexed as
Identifiers
What OpenQuestion holds
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.