ArticlePharmaceutical research2006
Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin.
Article in Pharmaceutical research, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 82 papers, 2 of them syntheses that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
82 citing papers in PubMed, 2 syntheses or guidelines pooled it, 194 citations in OpenAlex.
- The relation between Parkinson's disease and non-steroidal anti-inflammatories; a systematic review and meta-analysis.Frontiers in pharmacology · 2024Pooled it
- NSAID use and the risk of Parkinson's disease: systematic review and meta-analysis of observational studies.Drugs & aging · 2009Pooled it
- Impact of ibuprofen and peroxisome proliferator-activated receptor gamma on emotion-related neural activation: A randomized, placebo-controlled trial.Brain, behavior, and immunity · 2021Trial
- Effect of Ibuprofen on BrainAGE: A Randomized, Placebo-Controlled, Dose-Response Exploratory Study.Biological psychiatry. Cognitive neuroscience and neuroimaging · 2018Trial
- Effects of prophylactic ibuprofen and paracetamol administration on the immunogenicity and reactogenicity of the 10-valent pneumococcal non-typeable Haemophilus influenzae protein D conjugated vaccine (PHiD-CV) co-administered with DTPa-combined vaccines in children: An open-label, randomized, controlled, non-inferiority trial.Human vaccines & immunotherapeutics · 2017Trial
- Postoperative analgesic effect of preoperative intravenous flurbiprofen in arthroscopic rotator cuff repair.Journal of anesthesia · 2009Trial
- Cyclooxygenase-mediated IL-10Rα signaling underlies pro-tumor phenotypes of macrophages in glioma.Cell death & disease · 2026Article
- The Activation of Aldehyde Dehydrogenase 2 (ALDH2) by Alda-1 and Flurbiprofen as a Common Mechanism to Reduce Alcohol Intake in Rats.International journal of molecular sciences · 2026Article
- Ubrogepant Plasma and Cerebrospinal Fluid Exposures in Participants With a History of Migraine: Findings From a Phase 1b Open-Label Trial.Clinical and translational science · 2026Article
- Article
- Hypothalamic Prostaglandins Facilitate Recovery From Severe Hypoglycemia but Exacerbate Recurrent Hypoglycemia in Mice.Diabetes · 2025Article
- PEGylated PLGA nanoparticles: unlocking advanced strategies for cancer therapy.Molecular cancer · 2025Review
- Ibuprofen Does Not Prevent Inhibition of Fetal Breathing Movements Caused by Intrauterine Inflammation in Fetal Sheep.International journal of molecular sciences · 2025Article
- Repeated Administrations of Polyphenolic Extracts Prevent Chronic Reflexive and Non-Reflexive Neuropathic Pain Responses by Modulating Gliosis and CCL2-CCR2/CX3CL1-CX3CR1 Signaling in Spinal Cord-Injured Female Mice.International journal of molecular sciences · 2025Article
- Brain endothelial permeability, transport, and flow assessed over 10 orders of magnitude using the in situ brain perfusion technique.Fluids and barriers of the CNS · 2024Article
- Lipopolysaccharide-mediated effects of the microbiota on sleep and body temperature.Scientific reports · 2024Article
- Assessing Blood-brain Barrier Function in the Context of Pain Management.Central nervous system agents in medicinal chemistry · 2024Review
- Prenatal and postnatal drug exposure: focus on persistent central effects.Neural regeneration research · 2023Review
- Structure-Guided Design ofInternational journal of molecular sciences · 2023Article
- Review
22 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
purposeTo determine the roles of blood-brain barrier (BBB) transport and plasma protein binding in brain uptake of nonsteroidal anti-inflammatory drugs (NSAIDs)-ibuprofen, flurbiprofen, and indomethacin.
methodsBrain uptake was measured using in situ rat brain perfusion technique.
results[14C]Ibuprofen, [3H]flurbiprofen, and [14C]indomethacin were rapidly taken up into the brain in the absence of plasma protein with BBB permeability-surface area products (PS(u)) to free drug of (2.63 +/- 0.11) x 10(-2), (1.60 +/- 0.08) x 10(-2), and (0.64 +/- 0.05) x 10(-2) mL s(-1) g(-1) (n = 9-11), respectively. BBB [14C]ibuprofen uptake was inhibited by unlabeled ibuprofen (Km = 0.85 +/- 0.02 mM, Vmax = 13.5 +/- 0.4 nmol s(-1) g(-1)) and indomethacin, but not by pyruvate, probenecid, digoxin, or valproate. No evidence was found for saturable BBB uptake of [3H]flurbiprofen or [14C]indomethacin. Initial brain uptake for all three NSAIDs was reduced by the addition of albumin to the perfusion buffer. The magnitude of the brain uptake reduction correlated with the NSAID free fraction in the perfusate.
conclusionsFree ibuprofen, flurbiprofen, and indomethacin rapidly cross the BBB, with ibuprofen exhibiting a saturable component of transport. Plasma protein binding limits brain NSAID uptake by reducing the free fraction of NSAID in the circulation.
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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.