ArticleJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism2015
Blocking of fatty acid amide hydrolase activity with PF-04457845 in human brain: a positron emission tomography study with the novel radioligand [(11)C]CURB.
Article in Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 39 citations in OpenAlex.
- PET imaging of FAAH in chronic Cannabis users: longitudinal assessment during short-term abstinence.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Endocannabinoid Modulation in Headache: Mechanisms, Models, and Translational Therapies.Cells · 2026Review
- Quantification of [Frontiers in neuroscience · 2026Article
- A preliminary investigation of tobacco co-use on endocannabinoid activity in people with cannabis use.Drug and alcohol dependence reports · 2025Article
- Fatty acid amide hydrolase in major depressive episodes: A [Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Mitigation of cisplatin-induced acute kidney injury through oral administration of fatty acid amide hydrolase inhibitor PF-04457845.The Journal of pharmacology and experimental therapeutics · 2025Article
- Impact of Childhood Trauma Exposure, Genetic Variation in Endocannabinoid Signaling, and Anxiety on Frontolimbic Pathways in Children.Cannabis and cannabinoid research · 2023Article
- Endocannabinoid System Biomarkers in Alzheimer's Disease.Cannabis and cannabinoid research · 2023Article
- Fatty acid amide hydrolase levels in brain linked with threat-related amygdala activation.Neuroimage. Reports · 2022Article
- On the Biomedical Properties of Endocannabinoid Degradation and Reuptake Inhibitors: Pre-clinical and Clinical Evidence.Neurotoxicity research · 2021Review
- Fatty acid amide hydrolase binding is inversely correlated with amygdalar functional connectivity: a combined positron emission tomography and magnetic resonance imaging study in healthy individuals.Journal of psychiatry & neuroscience : JPN · 2021Article
- Fatty acid amide hydrolase is lower in young cannabis users.Addiction biology · 2021Article
- Endocannabinoids and Precision Medicine for Mood Disorders and Suicide.Frontiers in psychiatry · 2021Article
- Imaging Brain Fatty Acid Amide Hydrolase in Untreated Patients With Psychosis.Biological psychiatry · 2020Article
- Lower brain fatty acid amide hydrolase in treatment-seeking patients with alcohol use disorder: a positron emission tomography study with [C-11]CURB.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2020Article
- Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development.European journal of nuclear medicine and molecular imaging · 2020Review
- Endocannabinoid signaling in psychiatric disorders: a review of positron emission tomography studies.Acta pharmacologica Sinica · 2019Review
- Article
- Using molecular imaging to understand early schizophrenia-related psychosis neurochemistry: a review of human studies.International review of psychiatry (Abingdon, England) · 2017Review
- Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Positron emission tomography with [(11)C]CURB was recently developed to quantify fatty acid amide hydrolase (FAAH), the enzyme responsible for hydrolyzing the endocannabinoid anandamide. This study investigated the test-retest reliability of [(11)C]CURB as well as its in vivo specificity and the validity of the kinetic model by using the highly specific FAAH inhibitor, PF-04457845. Five healthy volunteers completed test-retest [(11)C]CURB scans 1 to 2 months apart and six subjects completed baseline and blocking scans on the same day after PF-04457845 (p.o.) administration (1, 4, or 20 mg; n=2 each). The composite parameter λk3 (an index of FAAH activity, λ=K1/k2) was estimated using an irreversible two-tissue compartment model with plasma input function. There were no clinically observable responses to oral PF-04457845 or [(11)C]CURB injection. Oral administration of PF-04457845 reduced [(11)C]CURB binding to a homogeneous level at all three doses, with λk3 values decreased by ⩾91%. Excellent reproducibility and good reliability (test-retest variability=9%; intraclass correlation coefficient=0.79) were observed across all regions of interest investigated. Our findings suggest that λk3/[(11)C]CURB is a reliable, highly sensitive, and selective tool to measure FAAH activity in human brain in vivo. Moreover, PF-04457845 is a highly potent FAAH inhibitor (>95% inhibition at 1 mg) in living human brain.
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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.