ArticleNuclear medicine and biology2010
High-resolution imaging of brain 5-HT 1B receptors in the rhesus monkey using [11C]P943.
Article in Nuclear medicine and biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 41 citations in OpenAlex.
- Age effects on serotonin receptor 1B as assessed by PET.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2012Trial
- In Vivo Imaging and Kinetic Modeling of Novel Glycogen Synthase Kinase-3 Radiotracers [Pharmaceuticals (Basel, Switzerland) · 2023Article
- Inverse changes in raphe and cortical 5-HTSynapse (New York, N.Y.) · 2020Article
- Article
- From simultaneous to synergistic MR-PET brain imaging: A review of hybrid MR-PET imaging methodologies.Human brain mapping · 2018Review
- Functional Characterization of 5-HTThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2017Article
- OCD is associated with an altered association between sensorimotor gating and cortical and subcortical 5-HT1b receptor binding.Journal of affective disorders · 2016Article
- Test-retest reliability of the novel 5-HT1B receptor PET radioligand [11C]P943.European journal of nuclear medicine and molecular imaging · 2015Article
- 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
- PET tracers for serotonin receptors and their applications.Central nervous system agents in medicinal chemistry · 2014Review
- Determination of the in vivo selectivity of a new κ-opioid receptor antagonist PET tracer 11C-LY2795050 in the rhesus monkey.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Article
- Serotonin 1B receptor imaging in pathological gambling.The world journal of biological psychiatry : the official journal of the World Federation of Societies of Biological Psychiatry · 2013Article
- Synthesis and evaluation of 11C-LY2795050 as a κ-opioid receptor antagonist radiotracer for PET imaging.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Article
- Molecular Neurobiology of Depression: PET Findings on the Elusive Correlation with Symptom Severity.Frontiers in psychiatry · 2013Article
- 5-HT radioligands for human brain imaging with PET and SPECT.Medicinal research reviews · 2013Review
- Optimization of PET-MR registrations for nonhuman primates using mutual information measures: a Multi-Transform Method (MTM).NeuroImage · 2013Article
- Assessing the sensitivity of [¹¹C]p943, a novel 5-HT1B radioligand, to endogenous serotonin release.Synapse (New York, N.Y.) · 2011Article
- The effect of early trauma exposure on serotonin type 1B receptor expression revealed by reduced selective radioligand binding.Archives of general psychiatry · 2011Article
- Evaluation of [(11)C]MRB for assessment of occupancy of norepinephrine transporters: Studies with atomoxetine in non-human primates.NeuroImage · 2011Article
- Reduced ventral striatal/ventral pallidal serotonin1B receptor binding potential in major depressive disorder.Psychopharmacology · 2011Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
The serotonin 5-HT(1B) receptors regulate the release of serotonin and are involved in various disease states, including depression and schizophrenia. The goal of the study was to evaluate a high affinity and high selectivity antagonist, [(11)C]P943, as a positron emission tomography (PET) tracer for imaging the 5-HT(1B) receptor. [(11)C]P943 was synthesized via N-methylation of the precursor with [(11)C]methyl iodide or [(11)C]methyl triflate using automated modules. The average radiochemical yield was approx. 10% with radiochemical purity of >99% and specific activity of 8.8+/-3.6 mCi/nmol at the end-of-synthesis (n=37). PET imaging was performed in non-human primates with a high-resolution research tomograph scanner with a bolus/infusion paradigm. Binding potential (BP(ND)) was calculated using the equilibrium ratios of regions to cerebellum. The tracer uptake was highest in the globus pallidus and occipital cortex, moderate in basal ganglia and thalamus, and lowest in the cerebellum, which is consistent with the known brain distribution of 5-HT(1B) receptors. Infusion of tracer at different specific activities (by adding various amount of unlabeled P943) reduced BP(ND) values in a dose-dependent manner, demonstrating the saturability of the tracer binding. Blocking studies with GR127935 (2 mg/kg iv), a selective 5-HT(1B)/5-HT(1D) antagonist, resulted in reduction of BP(ND) values by 42-95% across regions; for an example, in occipital region from 0.71 to 0.03, indicating a complete blockade. These results demonstrate the saturability and specificity of [(11)C]P943 for 5-HT(1B) receptors, suggesting its suitability as a PET radiotracer for in vivo evaluations of the 5-HT(1B) receptor system in humans.
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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.