ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2016
Occupancy of Dopamine D3 and D2 Receptors by Buspirone: A [11C]-(+)-PHNO PET Study in Humans.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 32 citations in OpenAlex.
- The behavioural effects of the serotonin 1A receptor agonist buspirone on cognition and emotional processing in healthy volunteers.Psychopharmacology · 2025Trial
- Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)-VK4-116, as a Non-Opioid Medication for the Treatment of Opioid Use Disorder.Medicinal research reviews · 2026Review
- Integrated bioinformatics and interaction analysis to advance chronotherapies for mental disorders.Frontiers in pharmacology · 2024Article
- The Anxiolytic Drug Buspirone Prevents Rotenone-Induced Toxicity in a Mouse Model of Parkinson's Disease.International journal of molecular sciences · 2022Article
- Dopamine Receptors: Is It Possible to Become a Therapeutic Target for Depression?Frontiers in pharmacology · 2022Review
- Article
- Evaluation of dopamine DPsychopharmacology · 2021Article
- Dopamine D3 receptor-based medication development for the treatment of opioid use disorder: Rationale, progress, and challenges.Neuroscience and biobehavioral reviews · 2020Review
- Separating dopamine DNeuroImage · 2020Article
- D3 dopamine receptors and a missense mutation of fatty acid amide hydrolase linked in mouse and men: implication for addiction.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2020Article
- Occupancy of dopamine DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2019Article
- Mining the Potential of Label-Free Biosensors for In Vitro Antipsychotic Drug Screening.Biosensors · 2018Article
- The effects of buspirone on occupancy of dopamine receptors and the rat gambling task.Psychopharmacology · 2017Article
- Development of molecular tools based on the dopamine DBioorganic & medicinal chemistry · 2017Article
- In Vitro and In Vivo Characterization of Selected Fluorine-18 Labeled Radioligands for PET Imaging of the Dopamine D3 Receptor.Molecules (Basel, Switzerland) · 2016Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
Abstract
There is considerable interest in blocking the dopamine D3 receptor (DRD3) versus the D2 receptor (DRD2) to treat drug addiction. However, there are currently no selective DRD3 antagonists available in the clinic. The anxiolytic drug buspirone has been proposed as a potential strategy as findings suggest that this drug has high in vitro affinity for DRD3, binds to DRD3 in brain of living non-human primate, and also disrupts psychostimulant self-administration in preclinical models. No study has explored the occupancy of DRD3 by buspirone in humans. Here, we used positron emission tomography (PET) and the D3-preferring probe, [(11)C]-(+)-PHNO, to test the hypothesis that buspirone will occupy (decreases [(11)C]-(+)-PHNO binding) the DRD3 more readily than the DRD2. Eight healthy participants underwent [(11)C]-(+)-PHNO scans after single oral dose administration of placebo and 30, 60, and 120 mg of buspirone in a single-blind within-subjects design. [(11)C]-(+)-PHNO binding in DRD2- and DRD3-rich areas was decreased by the highest (60-120 mg), but not the lowest (30 mg), doses of buspirone. The maximal occupancy obtained was ~25% in both areas. Plasma levels of prolactin (a DRD2 marker) correlated with percentage occupancy after orally administered buspirone. Self-reported dizziness and drowsiness increased after buspirone but that did not correlate with receptor occupancy in any region. Overall, the modest occupancy of DRD2 and DRD3 even at high acute doses of buspirone, yielding high levels of metabolites, suggests that buspirone may not be a good drug to preferentially block DRD3 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.