Human Brain Imaging and Radiation Dosimetry of 11C-N-Desmethyl-Loperamide, a PET Radiotracer to Measure the Function of P-Glycoprotein

No abstract is available for this paper.

• Publication year

  2009

• Venue

  Journal of Nuclear Medicine

• Publication date

  2009-05-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.2967/jnumed.108.058453PMID 19372478PMCID PMC2792991
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• 11C-Loperamide and Its N-Desmethyl Radiometabolite Are Avid Substrates for Brain Permeability-Glycoprotein Efflux

  2008cited by this paper
• P-Glycoprotein Function at the Blood–Brain Barrier Imaged Using 11C-N-Desmethyl-Loperamide in Monkeys

  2008cited by this paper
• The role of P-glycoprotein on blood brain barrier permeability of [11C]Loperamide in humans

  2008cited by this paper
• Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.

  2008cited by this paper
• Whole-body biodistribution and radiation dosimetry in monkeys and humans of the phosphodiesterase 4 radioligand [(11)C](R)-rolipram: comparison of two-dimensional planar, bisected and quadrisected image analyses.

  2008cited by this paper
• Human biodistribution and radiation dosimetry of the tachykinin NK1 antagonist radioligand [18F]SPA-RQ: comparison of thin-slice, bisected, and 2-dimensional planar image analysis.

  2007cited by this paper
• Evaluation of Tracer Kinetic Models for Quantification of P-Glycoprotein Function using (R)-[11C]Verapamil and PET

  2007cited by this paper
• Radiation Dosimetry and Biodistribution in Monkey and Man of 11C-PBR28: A PET Radioligand to Image Inflammation

  2007cited by this paper
• Quantitative analysis of 11C-verapamil transfer at the human blood-brain barrier for evaluation of P-glycoprotein function.

  2006cited by this paper
• PET imaging of the dopamine transporter with 18F-FECNT: a polar radiometabolite confounds brain radioligand measurements.

  2006cited by this paper
• In Vivo Evaluation of P-glycoprotein Function at the Blood-Brain Barrier in Nonhuman Primates Using [11C]Verapamil

  2006cited by this paper
• PRODUCTION OF THE P-GLYCOPROTEIN MARKER, [C-11]LOPERAMIDE, IN CLINICALLY USEFUL QUANTITIES

  2005cited by this paper
• Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi

  2005influential reference
• OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine.

  2005cited by this paper
• Evaluation of (R)-[11C]verapamil as PET tracer of P-glycoprotein function in the blood-brain barrier: kinetics and metabolism in the rat.

  2005cited by this paper
• Importance of P-glycoprotein at blood-tissue barriers.

  2004cited by this paper
• Biodistribution, radiation dose estimates, and in vivo Pgp modulation studies of 18F-paclitaxel in nonhuman primates.

  2003cited by this paper
• Basic anatomical and physiological data for use in radiological protection: reference values

  2002cited by this paper
• Evaluation of ultrafiltration for the free-fraction determination of single photon emission computed tomography (SPECT) radiotracers: beta-CIT, IBF, and iomazenil.

  1994cited by this paper
• Functional imaging of multidrug-resistant P-glycoprotein with an organotechnetium complex.

  1993cited by this paper

• Designing a Small Molecule for PET Radiotracing: [18F]MC225 in Human Trials for Early Diagnosis in CNS Pathologies

  2025influential citation
• [18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors.

  2025cites this paper
• Performance and Sensitivity of [99mTc]Tc-sestamibi Compared with Positron Emission Tomography Radiotracers to Measure P-glycoprotein Function in the Kidneys and Liver

  2024cites this paper
• Cardiac PET Imaging of ATP Binding Cassette (ABC) Transporters: Opportunities and Challenges

  2023cites this paper
• The Tetrahydroisoquinoline Scaffold in ABC Transporter Inhibitors that Act as Multidrug Resistance (MDR) Reversers.

  2022cites this paper
• Brain exposure of the ATM inhibitor AZD1390 in humans—a positron emission tomography study

  2021cites this paper
• Neuroimaging in Psychiatric Drug Development and Radioligand Development for New Targets

  2020cites this paper
• The Role of P-Glycoprotein at the Blood–Brain Barrier in Neurological and Psychiatric Disease

  2020cites this paper
• Brain exposure of the ATM inhibitor AZD1390 in humans - a positron emission tomography (PET) study.

  2020cites this paper
• [PET imaging to study the functional impact of P-glycoprotein in neuropharmacokinetics].

  2020cites this paper
• Nuclear Medicine Imaging Tracers for Neurology

  2020cites this paper
• A Practical Perspective on the Evaluation of Small Molecule CNS Penetration in Drug Discovery.

  2020cites this paper
• Advanced Mass Spectrometry Imaging in Neuropharmacology

  2019cites this paper
• Biomarkers of Drug Response and Pharmacoresistance to Epilepsy

  2019cites this paper
• A mass spectrometry imaging approach for investigating how drug‐drug interactions influence drug blood‐brain barrier permeability

  2018influential citation
• Revisiting the role of ABC transporters in multidrug-resistant cancer

  2018cites this paper
• [11C]phenytoin quantification

  2017cites this paper
• Chapter 5 [ 11 C ] phenytoin quantification

  2017cites this paper
• Kinetic Models for Measuring P-glycoprotein Function at the Blood-Brain Barrier with Positron Emission Tomography.

  2016cites this paper
• A multimodal Pepstatin A peptide-based nanoagent for the molecular imaging of P-glycoprotein in the brains of epilepsy rats.

  2016cites this paper
• ABC Transporters and Drug Resistance in Patients with Epilepsy.

  2016cites this paper
• Advances of Molecular Imaging in Epilepsy

  2016cites this paper
• Factors Governing P-Glycoprotein-Mediated Drug–Drug Interactions at the Blood–Brain Barrier Measured with Positron Emission Tomography

  2015cites this paper
• Increased Permeability-Glycoprotein Inhibition at the Human Blood–Brain Barrier Can Be Safely Achieved by Performing PET During Peak Plasma Concentrations of Tariquidar

  2015influential citation
• Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment: A Positron Emission Tomography Imaging Study

  2015cites this paper
• Quantification of Dynamic 11C-Phenytoin PET Studies

  2015cites this paper
• Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment : a PET Imaging Study

  2015cites this paper
• Species Differences and Impact of Disease State on BBB

  2015cites this paper
• Mechanisms of regulation of P-glycoprotein and breast cancer resistance protein at the blood-brain barrier : focus on the role of morphine, and P-glycoprotein activation

  2015cites this paper
• PET Imaging of ABC Transporters in the BBB

  2014cites this paper
• The Role of P-Glycoprotein in Psychiatric Disorders and in Psychiatric Treatment

  2014cites this paper
• Increased P-gp inhibition at the human blood brain barrier can be safely achieved by performing PET during peak plasma concentrations of tariquidar

  2014cites this paper
• Human ABC transporters at blood-CNS interfaces as determinants of CNS drug penetration.

  2014cites this paper
• RETRACTED: Radiosynthesis of 18F-labeled N-desmethyl-loperamide analogues for prospective molecular imaging radiotracers

  2013cites this paper
• Impact of epilepsy and drug-responsiveness☆

  2013cites this paper
• A high-yield route to synthesize the P-glycoprotein radioligand [11C]N-desmethyl-loperamide and its parent radioligand [11C]loperamide.

  2013cites this paper
• Physiologically Based Pharmacokinetic Modelling of Drug Penetration Across the Blood–Brain Barrier—Towards a Mechanistic IVIVE-Based Approach

  2013cites this paper
• Advances in PET imaging of P-glycoprotein function at the blood-brain barrier.

  2013cites this paper
• [11C]quinidine and [11C]laniquidar PET imaging in a chronic rodent epilepsy model: impact of epilepsy and drug-responsiveness.

  2013cites this paper
• Imaging P-glycoprotein function in rats using [11C]-N-desmethyl-loperamide

  2013cites this paper
• Whole-body distribution and radiation dosimetry of [11C]telmisartan as a biomarker for hepatic organic anion transporting polypeptide (OATP) 1B3.

  2012cites this paper
• Radiation dose estimates for carbon-11-labelled PET tracers.

  2012cites this paper
• Suggested pathway to assess radiation safety of 18F-labeled PET tracers for first-in-human studies

  2012cites this paper
• Reproducibility of quantitative (R)-[11C]verapamil studies

  2012cites this paper
• Evaluation of the near infrared compound indocyanine green as a probe substrate of p-glycoprotein.

  2012cites this paper
• ORIGINAL RESEARCH Open Access Reproducibility of quantitative (R)-( 11 C)verapamil

  2012cites this paper
• Increased In Vivo Expression of an Inflammatory Marker in Temporal Lobe Epilepsy

  2012cites this paper
• A Novel Positron Emission Tomography Imaging Protocol Identifies Seizure-Induced Regional Overactivity of P-Glycoprotein at the Blood–Brain Barrier

  2011influential citation
• P-glycoprotein at the blood-brain barrier: kinetic modeling of 11C-desmethylloperamide in mice using a 18F-FDG μPET scan to determine the input function

  2011cites this paper
• Suggested pathway to assess radiation safety of 11C-labeled PET tracers for first-in-human studies

  2011cites this paper
• Blood-brain barrier P-glycoprotein function in neurodegenerative disease.

  2011cites this paper
• ANovelPositronEmissionTomographyImagingProtocol IdentifiesSeizure-InducedRegionalOveractivityof P-GlycoproteinattheBlood-BrainBarrier

  2011cites this paper
• Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein).

  2011cites this paper
• Interplay of drug metabolizing CYP450 enzymes and ABC transporters in the blood-brain barrier.

  2011cites this paper
• Human biodistribution and radiation dosimetry of 11C-(R)-PK11195, the prototypic PET ligand to image inflammation

  2010cites this paper
• P-Glycoprotein Function at the Blood–Brain Barrier in Humans Can Be Quantified with the Substrate Radiotracer 11C-N-Desmethyl-Loperamide

  2010cites this paper
• Regional P‐Glycoprotein Activity and Inhibition at the Human Blood–Brain Barrier as Imaged by Positron Emission Tomography

  2010cites this paper
• P-glycoprotein related drug interactions: clinical importance and a consideration of disease states

  2010cites this paper
• Effects of ketoconazole on the biodistribution and metabolism of [11C]loperamide and [11C]N-desmethyl-loperamide in wild-type and P-gp knockout mice.

  2010cites this paper
• Drug delivery to the brain: considerations of genetic polymorphisms of blood-brain barrier transporters and imaging technologies.

  2010cites this paper
• Using PET studies of P-gp function to elucidate mechanisms underlying the disposition of drugs.

  2010cites this paper
• Radiosynthesis and in vivo evaluation of [(11)C]MC80 for P-glycoprotein imaging.

  2010cites this paper
• 11C-verapamil to assess P-gp function in human brain during aging, depression and neurodegenerative disease.

  2010cites this paper
• Evaluation of In Vivo P-Glycoprotein Phenotyping Probes

  2010cites this paper
• Substrates, inhibitors and activators of P-glycoprotein: candidates for radiolabeling and imaging perspectives.

  2010cites this paper
• Biodistribution and radiation dosimetry of [11C]choline: a comparison between rat and human data

  2010cites this paper
• Carbon-11 labeled tracers for in vivo imaging P-glycoprotein function: kinetics, advantages and disadvantages.

  2010cites this paper
• Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier.

  2009cites this paper
• PET radiotracers: crossing the blood-brain barrier and surviving metabolism.

  2009cites this paper
• Imaging the Function of P‐Glycoprotein With Radiotracers: Pharmacokinetics and In Vivo Applications

  2009cites this paper
• Summary and Discussion Summary and Discussion

  year unknowncites this paper