ArticleJournal of medicinal chemistry2014
Development of purine-derived 18F-labeled pro-drug tracers for imaging of MRP1 activity with PET.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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
9 citing papers in PubMed, 19 citations in OpenAlex.
- Measuring blood-brain barrier dysfunction: a critical appraisal of fluid biomarkers, in vitro models, in vivo imaging, and post-mortem approaches.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2026Review
- Discovery and in vivo evaluation of a fluorine-18 pro-drug tracer for imaging sphingosine-1-phosphate receptor 2 in the brain.Bioorganic & medicinal chemistry · 2026Article
- Synthesis and In Silico Profile Modeling of 6-International journal of molecular sciences · 2025Article
- Improved synthesis of 6-bromo-7-[EJNMMI radiopharmacy and chemistry · 2024Article
- A Medicinal Chemistry Perspective on Excitatory Amino Acid Transporter 2 Dysfunction in Neurodegenerative Diseases.Journal of medicinal chemistry · 2023Review
- GMBP1-conjugated manganese oxide nanoplates forRSC advances · 2020Article
- Manganese-Based Targeted Nanoparticles for Postoperative Gastric Cancer MonitoringFrontiers in oncology · 2020Article
- Evaluation of Enzyme Substrate Radiotracers as PET/MRS Hybrid Imaging Agents.ACS medicinal chemistry letters · 2018Article
- Alzheimer's and ABC transporters--new opportunities for diagnostics and treatment.Neurobiology of disease · 2014Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Multidrug resistance-associated protein 1 (MRP1) is a drug efflux transporter that has been implicated in the pathology of several neurological diseases and is associated with development of multidrug resistance. To enable measurement of MRP1 function in the living brain, a series of 6-halopurines decorated with fluorinated side chains have been synthesized and evaluated as putative pro-drug tracers. The tracers were designed to undergo conjugation with glutathione within the brain and hence form the corresponding MRP1 substrate tracers in situ. 6-Bromo-7-(2-[(18)F]fluoroethyl)purine showed good brain uptake and rapid metabolic conversion. Dynamic PET imaging demonstrated a marked difference in brain clearance rates between wild-type and mrp1 knockout mice, suggesting that the tracer can allow noninvasive assessment of MRP1 activity in vivo.
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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.