ArticlePsychopharmacology2012
Striatal and extrastriatal dopamine D₂ receptor occupancy by the partial agonist antipsychotic drug aripiprazole in the human brain: a positron emission tomography study with [¹¹C]raclopride and [¹¹C]FLB457.
Article in Psychopharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed, 24 citations in OpenAlex.
- An investigation into aripiprazole's partial D₂ agonist effects within the dorsolateral prefrontal cortex during working memory in healthy volunteers.Psychopharmacology · 2016Trial
- The sense and nonsense of antipsychotic combinations: A model for dopamine DTranslational psychiatry · 2025Article
- Association of protein distribution and gene expression revealed by positron emission tomography and postmortem gene expression in the dopaminergic system of the human brain.European journal of nuclear medicine and molecular imaging · 2023Article
- Molecular Imaging of Dopamine Partial Agonists in Humans: Implications for Clinical Practice.Frontiers in psychiatry · 2022Review
- Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity.Current neuropharmacology · 2017Article
- Short-term Effects of Risperidone Monotherapy on Spontaneous Brain Activity in First-episode Treatment-naïve Schizophrenia Patients: A Longitudinal fMRI Study.Scientific reports · 2016Article
- Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism.CNS drugs · 2015Review
- Antidepressant response to aripiprazole augmentation associated with enhanced FDOPA utilization in striatum: a preliminary PET study.Psychiatry research · 2014Article
- When to start aripiprazole therapy in patients with bipolar mania.Neuropsychiatric disease and treatment · 2014Review
- Effects of repeated treatment with the dopamine D2/D3 receptor partial agonist aripiprazole on striatal D2/D3 receptor availability in monkeys.Psychopharmacology · 2013Article
- Successful treatment of dopamine dysregulation syndrome with dopamine D2 partial agonist antipsychotic drug.Annals of general psychiatry · 2012Article
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15 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
rationaleSecond-generation antipsychotics demonstrate clinical efficacy with fewer extrapyramidal side effects compared with first-generation antipsychotics. One of the proposed explanations is the hypothesis of preferential extrastriatal dopamine D₂ receptor occupancy (limbic selectivity) by antipsychotics. In the present study, we focused on aripiprazole, which has a unique pharmacological profile with partial agonism at dopamine D₂ receptors and the minimal risk of extrapyramidal side effects. Previous positron emission tomography (PET) studies using high-affinity radioligands for dopamine D₂ receptors have reported inconsistent results regarding regional differences of dopamine D₂ receptor occupancy by aripiprazole.
objectiveTo test the hypothesis of preferential binding to extrastriatal dopamine D₂ receptors by aripiprazole, we investigated its regional dopamine D₂ receptor occupancies in healthy young subjects. MATERIALS AND
methodsUsing PET and two radioligands with different affinities for dopamine D₂ receptors, [¹¹C]raclopride and [¹¹C]FLB457, striatal and extrastriatal dopamine D₂ receptor bindings at baseline and after oral administration of 6 mg aripiprazole were measured in 11 male healthy subjects.
resultsOur data showed that dopamine D₂ receptor occupancies in the striatum measured with [¹¹C]raclopride were 70.1% and 74.1%, with the corresponding values for the extrastriatal regions measured with [¹¹C]FLB457 ranging from 46.6% to 58.4%.
conclusionsIn the present study, preferential extrastriatal dopamine D₂ receptor occupancy by aripiprazole was not observed. Our data suggest partial agonism at dopamine D₂ receptors is the most likely explanation for the minimal risk of extrapyramidal side effects in the treatment by aripiprazole.
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