ArticleEpilepsy research2012
The antiepileptic drug mephobarbital is not transported by P-glycoprotein or multidrug resistance protein 1 at the blood-brain barrier: a positron emission tomography study.
Article in Epilepsy research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The trial behind it
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Who cites it
8 citing papers in PubMed, 12 citations in OpenAlex.
- Drug-resistant Epilepsy: Which Drugs are Substrates of P-glycoprotein and Which are Not?Current neuropharmacology · 2026Review
- Multiple drug transporters contribute to the brain transfer of levofloxacin.CNS neuroscience & therapeutics · 2023Article
- Recent update on barbiturate in relation to brain disorder.EXCLI journal · 2021Article
- Altered Function and Expression of ABC Transporters at the Blood-Brain Barrier and Increased Brain Distribution of Phenobarbital in Acute Liver Failure Mice.Frontiers in pharmacology · 2018Article
- Drug-Resistant Epilepsy: Multiple Hypotheses, Few Answers.Frontiers in neurology · 2017Review
- Development and performance test of an online blood sampling system for determination of the arterial input function in rats.EJNMMI physics · 2015Article
- A proposed role for efflux transporters in the pathogenesis of hydrocephalus.Croatian medical journal · 2014Review
- Advances in PET imaging of P-glycoprotein function at the blood-brain barrier.ACS chemical neuroscience · 2013Review
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 2 countries.
Funding
Abstract
Aim of this study was to determine whether the carbon-11-labeled antiepileptic drug [(11)C]mephobarbital is a substrate of P-glycoprotein (Pgp) and can be used to assess Pgp function at the blood-brain barrier (BBB) with positron emission tomography (PET). We performed paired PET scans in rats, wild-type (FVB) and Mdr1a/b((-/-)) mice, before and after intravenous administration of the Pgp inhibitor tariquidar (15mg/kg). Brain-to-blood AUC(0-60) ratios in rats and brain AUC(0-60) values of [(11)C]mephobarbital in wild-type and Mdr1a/b((-/-)) mice were similar in scans 1 and 2, respectively, suggesting that in vivo brain distribution of [(11)C]mephobarbital is not influenced by Pgp efflux. Absence of Pgp transport was confirmed in vitro by performing concentration equilibrium transport assay in cell lines transfected with MDR1 or Mdr1a. PET experiments in wild-type mice, with and without pretreatment with the multidrug resistance protein (MRP) inhibitor MK571 (20mg/kg), and in Mrp1((-/-)) mice suggested that [(11)C]mephobarbital is also not transported by MRPs at the murine BBB, which was also supported by in vitro transport experiments using human MRP1-transfected cells. Our results are surprising, as phenobarbital, the N-desmethyl derivative of mephobarbital, has been shown to be a substrate of Pgp, which suggests that N-methylation abolishes Pgp affinity of barbiturates.
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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.