ArticleJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism2012
A novel PET protocol for visualization of breast cancer resistance protein function at the blood-brain barrier.
Article in Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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.
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Who cites it
27 citing papers in PubMed, 51 citations in OpenAlex.
- Interaction of 11C-tariquidar and 11C-elacridar with P-glycoprotein and breast cancer resistance protein at the human blood-brain barrier.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Trial
- Evaluating methodological constraints in PET imaging of neuropeptide Y2 receptors with N-[EJNMMI radiopharmacy and chemistry · 2025Article
- The ATP-Binding Cassette Transporter-Mediated Efflux Transport of Ganciclovir at the Blood-Brain Barrier.European journal of drug metabolism and pharmacokinetics · 2024Article
- Implications of BCRP modulation on PTZ-induced seizures in mice: Role of ko143 and metformin as adjuvants to lamotrigine.Naunyn-Schmiedeberg's archives of pharmacology · 2023Article
- Multiple drug transporters contribute to the brain transfer of levofloxacin.CNS neuroscience & therapeutics · 2023Article
- The Tetrahydroisoquinoline Scaffold in ABC Transporter Inhibitors that Act as Multidrug Resistance (MDR) Reversers.Current topics in medicinal chemistry · 2022Review
- Assessing the Functional Redundancy between P-gp and BCRP in Controlling the Brain Distribution and Biliary Excretion of Dual Substrates with PET Imaging in Mice.Pharmaceutics · 2021Article
- Complete inhibition of ABCB1 and ABCG2 at the blood-brain barrier by co-infusion of erlotinib and tariquidar to improve brain delivery of the model ABCB1/ABCG2 substrate [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021Article
- Brain Distribution of Dual ABCB1/ABCG2 Substrates Is Unaltered in a Beta-Amyloidosis Mouse Model.International journal of molecular sciences · 2020Article
- Novel Intrinsic Mechanisms of Active Drug Extrusion at the Blood-Brain Barrier: Potential Targets for Enhancing Drug Delivery to the Brain?Pharmaceutics · 2020Review
- Use of imaging to assess the activity of hepatic transporters.Expert opinion on drug metabolism & toxicology · 2020Review
- ABC Transporters at the Blood-Brain Interfaces, Their Study Models, and Drug Delivery Implications in Gliomas.Pharmaceutics · 2019Review
- Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration.European journal of drug metabolism and pharmacokinetics · 2018Article
- Synthesis, pharmacology and preclinical evaluation ofEuropean journal of medicinal chemistry · 2018Article
- Influence of breast cancer resistance protein and P-glycoprotein on tissue distribution and excretion of Ko143 assessed with PET imaging in mice.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2018Article
- Evaluation of [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- Altered GABAA receptor density and unaltered blood-brain barrier [11C]flumazenil transport in drug-resistant epilepsy patients with mesial temporal sclerosis.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- Noninvasive Evaluation of Cellular Proliferative Activity in Brain Neurogenic Regions in Rats under Depression and Treatment by Enhanced [18F]FLT-PET Imaging.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2016Article
- Pilot PET Study to Assess the Functional Interplay Between ABCB1 and ABCG2 at the Human Blood-Brain Barrier.Clinical pharmacology and therapeutics · 2016Article
- (67/68)Galmydar: A metalloprobe for monitoring breast cancer resistance protein (BCRP)-mediated functional transport activity.Nuclear medicine and biology · 2016Article
Corrections and comments
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
Abstract
Breast cancer resistance protein (BCRP) is the most abundant multidrug efflux transporter at the human blood-brain barrier (BBB), restricting brain distribution of various drugs. In this study, we developed a positron emission tomography (PET) protocol to visualize Bcrp function at the murine BBB, based on the dual P-glycoprotein (P-gp)/Bcrp substrate radiotracer [(11)C]tariquidar in combination with the Bcrp inhibitor Ko143. To eliminate the contribution of P-gp efflux to [(11)C]tariquidar brain distribution, we studied mice in which P-gp was genetically knocked out (Mdr1a/b((-/-)) mice) or chemically knocked out by pretreatment with cold tariquidar. We found that [(11)C]tariquidar brain uptake increased dose dependently after administration of escalating doses of Ko143, both in Mdr1a/b((-/-)) mice and in tariquidar pretreated wild-type mice. After 15 mg/kg Ko143, the maximum increase in [(11)C]tariquidar brain uptake relative to baseline scans was 6.3-fold in Mdr1a/b((-/-)) mice with a half-maximum effect dose of 4.98 mg/kg and 3.6-fold in tariquidar (8 mg/kg) pretreated wild-type mice, suggesting that the presented protocol is sensitive to visualize a range of different functional Bcrp activities at the murine BBB. We expect that this protocol can be translated to the clinic, because tariquidar can be safely administered to humans at doses that completely inhibit cerebral P-gp.
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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.