ArticleJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism2014
Imaging endogenous opioid peptide release with [11C]carfentanil and [3H]diprenorphine: influence of agonist-induced internalization.
Article 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 20 papers.
What it found
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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.
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Who cites it
20 citing papers in PubMed, 36 citations in OpenAlex.
- Blunted endogenous opioid release following an oral dexamphetamine challenge in abstinent alcohol-dependent individuals.Molecular psychiatry · 2020Trial
- Review
- Exceptional brain PET images from the NeuroEXPLORER: scans with targeted radiopharmaceuticals and comparison to HRRT.European journal of nuclear medicine and molecular imaging · 2026Article
- Investigation of [Scientific reports · 2024Article
- Article
- Naloxone's dose-dependent displacement of [Scientific reports · 2022Article
- Seasonal Variation in the Brain μ-Opioid Receptor Availability.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2021Article
- Medications Development for Treatment of Opioid Use Disorder.Cold Spring Harbor perspectives in medicine · 2021Review
- Pharmacological Characterization of Low-to-Moderate Affinity Opioid Receptor Agonists and Brain Imaging withJournal of medicinal chemistry · 2020Article
- A Survey of Molecular Imaging of Opioid Receptors.Molecules (Basel, Switzerland) · 2019Review
- Reduced mu opioid receptor availability in schizophrenia revealed with [Nature communications · 2019Article
- 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
- Opioid system and human emotions.British journal of pharmacology · 2018Review
- The pharmacology of amphetamine and methylphenidate: Relevance to the neurobiology of attention-deficit/hyperactivity disorder and other psychiatric comorbidities.Neuroscience and biobehavioral reviews · 2018Review
- Molecular and functional PET-fMRI measures of placebo analgesia in episodic migraine: Preliminary findings.NeuroImage. Clinical · 2018Article
- Deep brain stimulation of the periaqueductal gray releases endogenous opioids in humans.NeuroImage · 2017Article
- Suppressed Fat Appetite after Roux-en-Y Gastric Bypass Surgery Associates with Reduced Brain μ-opioid Receptor Availability in Diet-Induced Obese Male Rats.Frontiers in neuroscience · 2016Article
- Application of cross-species PET imaging to assess neurotransmitter release in brain.Psychopharmacology · 2015Review
- Endogenous Opioid Mechanisms Are Implicated in Obesity and Weight Loss in Humans.The Journal of clinical endocrinology and metabolism · 2015Article
- Positron emission tomography imaging of endogenous mu-opioid mechanisms during pain and migraine.Pain reportsReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Understanding the cellular processes underpinning the changes in binding observed during positron emission tomography neurotransmitter release studies may aid translation of these methodologies to other neurotransmitter systems. We compared the sensitivities of opioid receptor radioligands, carfentanil, and diprenorphine, to amphetamine-induced endogenous opioid peptide (EOP) release and methadone administration in the rat. We also investigated whether agonist-induced internalization was involved in reductions in observed binding using subcellular fractionation and confocal microscopy. After radioligand administration, significant reductions in [(11)C]carfentanil, but not [(3)H]diprenorphine, uptake were observed after methadone and amphetamine pretreatment. Subcellular fractionation and in vitro radioligand binding studies showed that amphetamine pretreatment only decreased total [(11)C]carfentanil binding. In vitro saturation binding studies conducted in buffers representative of the internalization pathway suggested that μ-receptors are significantly less able to bind the radioligands in endosomal compared with extracellular compartments. Finally, a significant increase in μ-receptor-early endosome co-localization in the hypothalamus was observed after amphetamine and methadone treatment using double-labeling confocal microscopy, with no changes in δ- or κ-receptor co-localization. These data indicate carfentanil may be superior to diprenorphine when imaging EOP release in vivo, and that alterations in the ability to bind internalized receptors may be a predictor of ligand sensitivity to endogenous neurotransmitter release.
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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.