ArticleThe international journal of neuropsychopharmacology2017
Occupancy of Norepinephrine Transporter by Duloxetine in Human Brains Measured by Positron Emission Tomography with (S,S)-[18F]FMeNER-D2.
Article in The international journal of neuropsychopharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 2 of them syntheses that pooled it.
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Who cites it
12 citing papers in PubMed, 2 syntheses or guidelines pooled it, 44 citations in OpenAlex.
- The relationship between dose and serotonin transporter occupancy of antidepressants-a systematic review.Molecular psychiatry · 2022Pooled it
- Item-based analysis of the effects of duloxetine in depression: a patient-level post hoc study.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2020Pooled it
- A longitudinal PET study on changes in brain norepinephrine transporter availability following duloxetine treatment in major depressive disorder.The international journal of neuropsychopharmacology · 2025Trial
- Trajectories of late-life depression: insights from molecular imaging.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Review
- Dose-Concentration Relationship and Clinical Outcomes of Duloxetine in Generalized Anxiety Disorder.Journal of clinical medicine · 2026Article
- Article
- Therapeutic reference range for duloxetine in the treatment of depression revised: A systematic review and meta-analysis.Neuroscience applied · 2024Review
- The utility of PET imaging in depression.Frontiers in psychiatry · 2024Review
- Adaptation of Lipid Profiling in Depression Disease and Treatment: A Critical Review.International journal of molecular sciences · 2022Review
- PET technology for drug development in psychiatry.Neuropsychopharmacology reports · 2020Review
- Recent advances in radiotracers targeting norepinephrine transporter: structural development and radiolabeling improvements.Journal of neural transmission (Vienna, Austria : 1996) · 2020Review
- Venlafaxine ER Blocks the Norepinephrine Transporter in the Brain of Patients with Major Depressive Disorder: a PET Study Using [18F]FMeNER-D2.The international journal of neuropsychopharmacology · 2019Article
Corrections and comments
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Authors and funding
15 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Background: The norepinephrine transporter in the brain has been targeted in the treatment of psychiatric disorders. Duloxetine is a serotonin and norepinephrine reuptake inhibitor that has been widely used for the treatment of depression. However, the relationship between dose and plasma concentration of duloxetine and norepinephrine transporter occupancy in the human brain has not been determined. In this study, we examined norepinephrine transporter occupancy by different doses of duloxetine. Methods: We calculated norepinephrine transporter occupancies from 2 positron emission tomography scans using (S,S)-[18F]FMeNER-D2 before and after a single oral dose of duloxetine (20 mg, n = 3; 40 mg, n = 3; 60 mg, n =2). Positron emission tomography scans were performed from 120 to 180 minutes after an i.v. bolus injection of (S,S)-[18F]FMeNER-D2. Venous blood samples were taken to measure the plasma concentration of duloxetine just before and after the second positron emission tomography scan. Results: Norepinephrine transporter occupancy by duloxetine was 29.7% at 20 mg, 30.5% at 40 mg, and 40.0% at 60 mg. The estimated dose of duloxetine inducing 50% norepinephrine transporter occupancy was 76.8 mg, and the estimated plasma drug concentration inducing 50% norepinephrine transporter occupancy was 58.0 ng/mL. Conclusions: Norepinephrine transporter occupancy by clinical doses of duloxetine was approximately 30% to 40% in human brain as estimated using positron emission tomography with (S,S)-[18F]FMeNER-D2.
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