ArticleEuropean journal of nuclear medicine and molecular imaging2010
Evaluation of the kappa-opioid receptor-selective tracer [(11)C]GR103545 in awake rhesus macaques.
Article in European journal of nuclear medicine and molecular imaging, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 35 citations in OpenAlex.
- Kinetic modeling of (11)C-LY2795050, a novel antagonist radiotracer for PET imaging of the kappa opioid receptor in humans.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2014Trial
- Article
- Optimization of a Nucleophilic Two-Step Radiosynthesis of 6-International journal of molecular sciences · 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
- 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
- Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging.Medicinal research reviews · 2019Review
- Is There a Role for GPCR Agonist Radiotracers in PET Neuroimaging?Frontiers in molecular neuroscience · 2019Review
- Kappa opioid receptor binding in major depression: A pilot study.Synapse (New York, N.Y.) · 2018Article
- Immediate and Persistent Effects of Salvinorin A on the Kappa Opioid Receptor in Rodents, Monitored In Vivo with PET.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2015Article
- μ and κ opioid receptor distribution in the monogamous titi monkey (Callicebus cupreus): implications for social behavior and endocrine functioning.Neuroscience · 2015Article
- Article
- An Improved Antagonist Radiotracer for the κ-Opioid Receptor: Synthesis and Characterization of (11)C-LY2459989.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2014Article
- Molecular imaging of conscious, unrestrained mice with AwakeSPECT.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Article
- Determination of in vivo Bmax and Kd for 11C-GR103545, an agonist PET tracer for κ-opioid receptors: a study in nonhuman primates.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Article
- The dynorphin/κ-opioid receptor system and its role in psychiatric disorders.Cellular and molecular life sciences : CMLS · 2012Review
- Mapping Kappa Opioid Receptor Binding in Titi Monkeys with [Molecular imagingArticle
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Authors and funding
12 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe recent development in radiosynthesis of the (11)C-carbamate function increases the potential of [(11)C]GR103545, which for the last decade has been regarded as promising for imaging the kappa-opioid receptor (kappa-OR) with PET. In the present study, [(11)C]GR103545 was evaluated in awake rhesus macaques. Separate investigations were performed to clarify the OR subtype selectivity of this compound.
methodsRegional brain uptake kinetics of [(11)C]GR103545 was studied 0-120 min after injection. The binding affinity and opioid subtype selectivity of [(11)C]GR103545 was determined in cells transfected with cloned human opioid receptors.
resultsIn vitro binding assays demonstrated a high affinity of GR103545 for kappa-OR (K(i) = 0.02 +/- 0.01 nM) with excellent selectivity over mu-OR (6 x 10(2)-fold) and) delta-OR (2 x 10(4)-fold). PET imaging revealed a volume of distribution (V(T)) pattern consistent with the known distribution of kappa-OR, with striatum = temporal cortex > cingulate cortex > frontal cortex > parietal cortex > thalamus > cerebellum.
conclusion[(11)C]GR103545 is selective for kappa-OR and holds promise for use to selectively depict and quantify this receptor in humans by means of PET.
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