ArticleClinical pharmacology and therapeutics2010
Regional P-glycoprotein activity and inhibition at the human blood-brain barrier as imaged by positron emission tomography.
Article in Clinical pharmacology and therapeutics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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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.
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Who cites it
36 citing papers in PubMed, 67 citations in OpenAlex.
- P-Glycoprotein and Breast Cancer Resistance Protein Transporter Inhibition by Cyclosporine and Quinidine on the Pharmacokinetics of Oral Rimegepant in Healthy Subjects.Clinical pharmacology in drug development · 2022Trial
- Positron Emission Tomography Imaging of [Clinical pharmacology and therapeutics · 2019Trial
- Impact of P-Glycoprotein Function on the Brain Kinetics of the Weak SubstrateJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Trial
- Approaching complete inhibition of P-glycoprotein at the human blood-brain barrier: an (R)-[11C]verapamil PET study.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2015Trial
- Pharmacogenetics of antidepressant response: a focused review on CYP2C19, CYP2D6, SLC6A4, and HTR2A polymorphisms.Frontiers in pharmacology · 2026Review
- Appraising the visibility, relevance and impacts of clinical pharmacology.British journal of clinical pharmacology · 2025Review
- Do P-glycoprotein-mediated drug-drug interactions at the blood-brain barrier impact morphine brain distribution?Journal of pharmacokinetics and pharmacodynamics · 2025Article
- PET in the characterization of immune diseases and development of therapeutics.Oxford open immunology · 2025Review
- Screening of medicinal plants for possible herb-drug interactions through modulating nuclear receptors, drug-metabolizing enzymes and transporters.Journal of ethnopharmacology · 2023Article
- Patient-Adaptive Population-Based Modeling of Arterial Input Functions.IEEE transactions on medical imaging · 2023Article
- Murine Central Nervous System and Bone Marrow Distribution of the Aurora A Kinase Inhibitor Alisertib: Pharmacokinetics and Exposure at the Sites of Efficacy and Toxicity.The Journal of pharmacology and experimental therapeutics · 2022Article
- Central Nervous System Delivery of the Catalytic Subunit of DNA-Dependent Protein Kinase Inhibitor Peposertib as Radiosensitizer for Brain Metastases.The Journal of pharmacology and experimental therapeutics · 2022Article
- Successful Prediction of Human Steady-State Unbound Brain-to-Plasma Concentration Ratio of P-gp Substrates Using the Proteomics-Informed Relative Expression Factor Approach.Clinical pharmacology and therapeutics · 2021Article
- Advancing Predictions of Tissue and Intracellular Drug Concentrations Using In Vitro, Imaging and Physiologically Based Pharmacokinetic Modeling Approaches.Clinical pharmacology and therapeutics · 2018Article
- Brain vascular heterogeneity: implications for disease pathogenesis and design of in vitro blood-brain barrier models.Fluids and barriers of the CNS · 2018Review
- Breaking Bad: the Structure and Function of the Blood-Brain Barrier in Epilepsy.The AAPS journal · 2017Review
- Pilot PET Study to Assess the Functional Interplay Between ABCB1 and ABCG2 at the Human Blood-Brain Barrier.Clinical pharmacology and therapeutics · 2016Article
- Advances of Molecular Imaging in Epilepsy.Current neurology and neuroscience reports · 2016Review
- Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment: A Positron Emission Tomography Imaging Study.Drug metabolism and disposition: the biological fate of chemicals · 2015Article
- Improved Antidepressant Remission in Major Depression via a Pharmacokinetic Pathway Polygene Pharmacogenetic Report.Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology · 2015Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
We used positron emission tomography (PET) to evaluate the contribution of P-glycoprotein (P-gp), present at the human blood-brain barrier (BBB), to regional drug distribution in the brain. Eleven healthy volunteers underwent PET imaging with [(11)C]-verapamil before and during cyclosporine A infusion. Regional P-gp inhibition was expressed as cyclosporine A-induced percentage change in the distributional clearance of verapamil (K(1)) in the brain, normalized to the regional blood flow (rCBF). K(1) estimates were similar across gray-matter regions of the brain and lower in the white matter regions, but all these estimates were considerably lower than rCBF. Normalization of K(1) by rCBF diminished the differences in estimates related to gray matter and white matter. In contrast, the K(1) for the pituitary, which is situated outside the BBB, approximated the rCBF. The magnitude of P-gp inhibition was comparable across BBB-protected brain structures. Our results indicate that P-gp and its inhibition equally affect the distribution of drugs (and therefore their neuro-efficacy and toxicity) in the various brain regions protected by the BBB.
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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.