ArticleThe international journal of neuropsychopharmacology2018
Comparison of Dopamine D3 and D2 Receptor Occupancies by a Single Dose of Blonanserin in Healthy Subjects: A Positron Emission Tomography Study With [11C]-(+)-PHNO.
Article in The international journal of neuropsychopharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 23 citations in OpenAlex.
- Association between treatment response and dose of blonanserin transdermal patch in patients with acute schizophrenia: A post hoc cluster analysis based on baseline psychiatric symptoms.Neuropsychopharmacology reports · 2024Trial
- Striatal Dopamine D2 Receptor Occupancy Induced by Daily Application of Blonanserin Transdermal Patches: Phase II Study in Japanese Patients With Schizophrenia.The international journal of neuropsychopharmacology · 2021Trial
- Blonanserin versus haloperidol in Japanese patients with schizophrenia: A phase 3, 8-week, double-blind, multicenter, randomized controlled study.Neuropsychopharmacology reports · 2019Trial
- Neu1 deficiency is associated with reduced nicotine responsiveness and dopamine D3 receptor downregulation in zebrafish.Fish physiology and biochemistry · 2026Article
- Clinical outcomes in first-episode schizophrenia: identifying predictors of relapse.Social psychiatry and psychiatric epidemiology · 2026Article
- Bilateral hand-restricted drug eruption induced by blonanserin: a case report.Frontiers in psychiatry · 2026Article
- D3 Receptor-Targeted Cariprazine: Insights from Lab to Bedside.International journal of molecular sciences · 2024Review
- Effect of scan-time shortening on theAnnals of nuclear medicine · 2023Article
- Potential Mechanisms for Why Not All Antipsychotics Are Able to Occupy Dopamine DFrontiers in psychiatry · 2022Review
- Long-term oral blonanserin treatment for schizophrenia: a review of Japanese long-term studies.Annals of general psychiatry · 2021Review
- Evaluation of dopamine DPsychopharmacology · 2021Article
- Multi-Atlas MRI-Based Striatum Segmentation forFrontiers in medicine · 2021Article
- Separating dopamine DNeuroImage · 2020Article
- PET technology for drug development in psychiatry.Neuropsychopharmacology reports · 2020Review
- Chronic treatment with the antipsychotic drug blonanserin modulates the responsiveness to acute stress with anatomical selectivity.Psychopharmacology · 2020Article
- Prediction of Corresponding Dose of Transdermal Blonanserin to Oral Dose Based on Dopamine D2 Receptor Occupancy: Unique Characteristics of Blonanserin Transdermal Patch.Journal of clinical psychopharmacologyArticle
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Background: Blockade of D3 receptor, a member of the dopamine D2-like receptor family, has been suggested as a possible medication for schizophrenia. Blonanserin has high affinity in vitro for D3 as well as D2 receptors. We investigated whether a single dose of 12 mg blonanserin, which was within the daily clinical dose range (i.e., 8-24 mg) for the treatment of schizophrenia, occupies D3 as well as D2 receptors in healthy subjects. Methods: Six healthy males (mean 35.7±7.6 years) received 2 positron emission tomography scans, the first prior to taking blonanserin, and the second 2 hours after the administration of a single dose of 12 mg blonanserin. Dopamine receptor occupancies by blonanserin were evaluated by [11C]-(+)-PHNO. Results: Occupancy of each region by 12 mg blonanserin was: caudate (range 64.3%-81.5%; mean±SD, 74.3±5.6%), putamen (range 60.4%-84.3%; mean±SD, 73.3%±8.2%), ventral striatum (range 40.1%-88.2%; mean±SD, 60.8%±17.1%), globus pallidus (range 65.8%-87.6%; mean±SD, 75.7%±8.6%), and substantia nigra (range 56.0%-88.7%; mean±SD, 72.4%±11.0%). Correlation analysis between plasma concentration of blonanserin and receptor occupancy in D2-rich (caudate and putamen) and D3-rich (globus pallidus and substantia nigra) regions showed that EC50 for D2-rich region was 0.39 ng/mL (r=0.43) and EC50 for D3-rich region was 0.40 ng/mL (r=0.79). Conclusions: A single dose of 12 mg blonanserin occupied D3 receptor to the same degree as D2 receptor in vivo. Our results were consistent with previous studies that reported that some of the pharmacological effect of blonanserin is mediated via D3 receptor antagonism.
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