ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2010
Impact of D2 receptor internalization on binding affinity of neuroimaging radiotracers.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers, 3 of them syntheses that pooled it.
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Who cites it
51 citing papers in PubMed, 3 syntheses or guidelines pooled it, 81 citations in OpenAlex.
- Association of Stimulant Use With Dopaminergic Alterations in Users of Cocaine, Amphetamine, or Methamphetamine: A Systematic Review and Meta-analysis.JAMA psychiatry · 2017Pooled it
- Striatal dopamine transporter availability in drug-naive patients with schizophrenia: a case-control SPECT study with [(99m)Tc]-TRODAT-1 and a meta-analysis.Schizophrenia bulletin · 2013Pooled it
- The nature of dopamine dysfunction in schizophrenia and what this means for treatment.Archives of general psychiatry · 2012Pooled it
- Dynamic alterations in the central glutamatergic status following food and glucose intake:Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021Trial
- The radiotracer [Annals of nuclear medicine · 2026Review
- Striatal spinophilin enhances dopamine D2 receptor (D2R) interaction with cytosolic proteins to mediate persistent D2R agonist-induced locomotor suppression.The Journal of pharmacology and experimental therapeutics · 2026Article
- Striatal spinophilin enhances D2R interaction with cytosolic proteins to mediate persistent D2R agonist-induced locomotor suppression.bioRxiv : the preprint server for biology · 2025Article
- Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Article
- Synaptotagmin-1-dependent phasic axonal dopamine release is dispensable for basic motor behaviors in mice.Nature communications · 2023Article
- Dopamine D3 Receptor in Parkinson Disease: A Prognosis Biomarker and an Intervention Target.Current topics in behavioral neurosciences · 2023Article
- Relationship between subjective well-being and aripiprazole: an [Scientific reports · 2022Article
- Dopamine D1R Receptor Stimulation as a Mechanistic Pro-cognitive Target for Schizophrenia.Schizophrenia bulletin · 2022Article
- Pharmacological perturbation reveals deficits in D2 receptor responses in Thap1 null mice.Annals of clinical and translational neurology · 2021Article
- A local-neighborhood Lassen plot filter for creating occupancy and non-displaceable binding images.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021Article
- Abnormal dopamine receptor signaling allows selective therapeutic targeting of neoplastic progenitors in AML patients.Cell reports. Medicine · 2021Article
- Measuring the effects of ketamine on mGluR5 using [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2020Article
- New roles for dopamine DMolecular psychiatry · 2020Article
- Dopamine and glutamate in schizophrenia: biology, symptoms and treatment.World psychiatry : official journal of the World Psychiatric Association (WPA) · 2020Article
- Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGluACS chemical neuroscience · 2019Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
Synaptic dopamine (DA) levels seem to affect the in vivo binding of many D2 receptor radioligands. Thus, release of endogenous DA induced by the administration of amphetamine decreases ligand binding, whereas DA depletion increases binding. This is generally thought to be due to competition between endogenous DA and the radioligands for D2 receptors. However, the temporal discrepancy between amphetamine-induced increases in DA as measured by microdialysis, which last on the order of 2 h, and the prolonged decrease in ligand binding, which lasts up to a day, has suggested that agonist-induced D2 receptor internalization may contribute to the sustained decrease in D2 receptor-binding potential seen following a DA surge. To test this hypothesis, we developed an in vitro system showing robust agonist-induced D2 receptor internalization following treatment with the agonist quinpirole. Human embryonic kidney 293 (HEK293) cells were stably co-transfected with human D2 receptor, G-protein-coupled receptor kinase 2 and arrestin 3. Agonist-induced D2 receptor internalization was demonstrated by fluorescence microscopy, flow cytometry, and radioligand competition binding. The binding of seven D2 antagonists and four agonists to the surface and internalized receptors was measured in intact cells. All the imaging ligands bound with high affinity to both surface and internalized D2 receptors. Affinity of most of the ligands to internalized receptors was modestly lower, indicating that internalization would reduce the binding potential measured in imaging studies carried out with these ligands. However, between-ligand differences in the magnitude of the internalization-associated affinity shift only partly accounted for the data obtained in neuroimaging experiments, suggesting the involvement of mechanisms beyond competition and internalization.
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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.