ArticleMolecular imaging and biology
Visualization and quantification of neurokinin-1 (NK1) receptors in the human brain.
Article in Molecular imaging and biology. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 64 citations in OpenAlex.
- Netupitant PET imaging and ADME studies in humans.Journal of clinical pharmacology · 2014Trial
- Imaging drugs with and without clinical analgesic efficacy.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2011Trial
- A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept trial.European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2011Trial
- Endocannabinoid signaling in stress, nausea, and vomiting.Neurogastroenterology and motility · 2025Review
- Functional evaluation of NKDrug and alcohol dependence · 2021Article
- [Scientific reports · 2019Article
- The Significance of NK1 Receptor Ligands and Their Application in Targeted Radionuclide Tumour Therapy.Pharmaceutics · 2019Review
- Association between amygdala neurokinin-1 receptor availability and anxiety-related personality traits.Translational psychiatry · 2018Article
- Overlapping expression of serotonin transporters and neurokinin-1 receptors in posttraumatic stress disorder: a multi-tracer PET study.Molecular psychiatry · 2016Article
- Design, Synthesis, and Evaluation of a Neurokinin-1 Receptor-Targeted Near-IR Dye for Fluorescence-Guided Surgery of Neuroendocrine Cancers.Bioconjugate chemistry · 2016Article
- Article
- The Therapeutic Potential of Targeting Substance P/NK-1R Interactions in Inflammatory CNS Disorders.Frontiers in cellular neuroscience · 2016Review
- Emerging drugs for the treatment of anxiety.Expert opinion on emerging drugs · 2015Review
- Increased neurokinin-1 receptor availability in the amygdala in social anxiety disorder: a positron emission tomography study with [11C]GR205171.Translational psychiatry · 2015Article
- The pharmacology of neurokinin receptors in addiction: prospects for therapy.Substance abuse and rehabilitation · 2015Review
- Quantification of central substance P receptor occupancy by aprepitant using small animal positron emission tomography.The international journal of neuropsychopharmacology · 2014Article
- Diminished neurokinin-1 receptor availability in patients with two forms of chronic visceral pain.Pain · 2013Article
- Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils.Behavioural pharmacology · 2009Article
- Prevention of acute chemotherapy-induced nausea and vomiting: the role of palonosetron.Cancer management and research · 2009Article
- Decreased neurokinin-1 (substance P) receptor binding in patients with panic disorder: positron emission tomographic study with [18F]SPA-RQ.Biological psychiatry · 2009Article
Corrections and comments
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Authors and funding
18 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThis study was conducted to develop a new positron emission tomography (PET) method to visualize neurokinin-1 (NK(1)) receptor systems in the human brain in vivo in order to examine their neuroanatomical distribution and facilitate investigations of the role of substance P, NK(1) receptors, and NK(1) receptor antagonists in central nervous system (CNS) function and dysfunction.
methodsPET studies were conducted in 10 healthy male volunteers using a novel selective, high-affinity NK(1) receptor antagonist labeled with fluorine-18 to very high specific radioactivity (up to 2000 GBq/micromol) [F-18]SPA-RQ. Data were collected in 3D mode for greatest sensitivity. Different modeling methods were compared and regional receptor distributions determined for comparison with in vitro autoradiographic studies using postmortem human brain slices with [F-18]SPA-RQ.
resultsThe studies showed that the highest uptake of [F-18]SPA-RQ was observed in the caudate and putamen. Lower binding was found in globus pallidus and substantia nigra. [F-18]SPA-RQ uptake was also widespread throughout the neocortex and limbic cortex including amygdala and hippocampus. There was very low specific uptake of the tracer in the cerebellar cortex. The distribution pattern was confirmed using in vitro receptor autoradiography with [F-18]SPA-RQ on postmortem human brain slices. Kinetic modeling of the [F-18]SPA-RQ uptake data indicated a binding potential between 4 and 5 in the basal ganglia and between 1.5 and 2.5 in the cortical regions.
conclusions[F-18]SPA-RQ is a novel tool for exploration of the functions of NK(1) receptors in man. [F-18]SPA-RQ can be used to define receptor pharmacodynamics and focus dose selection of novel NK(1) receptor antagonists in clinical trials thereby ensuring adequate proof of concept testing particularly in therapeutic applications related to CNS dysfunction.
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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.