Advances in PET imaging of P-glycoprotein function at the blood-brain barrier

scientific article published on 4 December 2012

Advances in PET imaging of P-glycoprotein function at the blood-brain barrier is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1021/CN3001729
P932PMC publication ID3582299
P698PubMed publication ID23421673

P2093author name stringJonas Eriksson
Stina Syvänen
P2860cites workSynthesis and preclinical evaluation of [11C]D617, a metabolite of (R)-[11C]verapamilQ48723948
Toward an improved prediction of human in vivo brain penetrationQ48852162
The influence of mass of [11C]-laniquidar and [11C]-N-desmethyl-loperamide on P-glycoprotein blockage at the blood-brain barrierQ48872323
Enhanced cerebral uptake of receptor ligands by modulation of P-glycoprotein function in the blood-brain barrierQ50108149
Blood-brain barrier P-glycoprotein function in Alzheimer's disease.Q50778486
Developmental changes in P-glycoprotein function in the blood-brain barrier of nonhuman primates: PET study with R-11C-verapamil and 11C-oseltamivir.Q51867355
Imaging multidrug resistance P-glycoprotein transport function using microPET with technetium-94m-sestamibi.Q53580923
Influence of P-glycoprotein on brain uptake of [18F]MPPF in ratsQ73163374
In vivo delineation of 5-HT1A receptors in human brain with [18F]MPPFQ73192746
Biodistribution, radiation dose estimates, and in vivo Pgp modulation studies of 18F-paclitaxel in nonhuman primatesQ73764953
Structure of P-glycoprotein reveals a molecular basis for poly-specific drug bindingQ24657908
Graphical evaluation of blood-to-brain transfer constants from multiple-time uptake dataQ28274520
(R)-[11C]verapamil PET studies to assess changes in P-glycoprotein expression and functionality in rat blood-brain barrier after exposure to kainate-induced status epilepticusQ30993837
beta-Amyloid efflux mediated by p-glycoproteinQ31962046
PET radiotracers: crossing the blood-brain barrier and surviving metabolismQ33585028
P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamideQ33797745
Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sitesQ33832954
Restoring blood-brain barrier P-glycoprotein reduces brain amyloid-beta in a mouse model of Alzheimer's diseaseQ33862071
Discrepancies in the P-glycoprotein-mediated transport of (18)F-MPPF: a pharmacokinetic study in mice and non-human primates.Q48490305
Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in ratsQ48496774
Kinetics and displacement of [11C]RO 15-1788, a benzodiazepine antagonist, studied in human brain in vivo by positron tomography.Q48496931
Effect of age on functional P-glycoprotein in the blood-brain barrier measured by use of (R)-[(11)C]verapamil and positron emission tomographyQ48502840
Evaluation of tracer kinetic models for quantification of P-glycoprotein function using (R)-[11C]verapamil and PET.Q48507860
Pharmacokinetic consequences of active drug efflux at the blood-brain barrierQ48598406
Estimates of Michaelis-Menten constants for the two membranes of the brain endotheliumQ48660778
A new in vivo method to study P-glycoprotein transport in tumors and the blood-brain barrierQ33863406
N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrierQ33891067
New positron emission tomography tracer [(11)C]carvedilol reveals P-glycoprotein modulation kineticsQ33987752
Drug resistance in brain diseases and the role of drug efflux transporters.Q33988704
11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein effluxQ34010493
Species differences in blood-brain barrier transport of three positron emission tomography radioligands with emphasis on P-glycoprotein transportQ34014920
Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeabilityQ34057451
Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomographyQ34067336
Pgp-mediated interaction between (R)-[11C]verapamil and tariquidar at the human blood-brain barrier: a comparison with rat dataQ34100185
Serotonin 5HT2 receptor imaging in the human brain using positron emission tomography and a new radioligand, [18F]altanserin: results in young normal controlsQ34305236
Positron emission tomography compartmental modelsQ34327907
Models and methods for derivation of in vivo neuroreceptor parameters with PET and SPECT reversible radiotracersQ34343207
Graphical analysis of reversible radioligand binding from time-activity measurements applied to [N-11C-methyl]-(-)-cocaine PET studies in human subjectsQ34356874
Brain distribution of cetirizine enantiomers: comparison of three different tissue-to-plasma partition coefficients: K(p), K(p,u), and K(p,uu).Q34469599
Review of immunological and immunopathological findings in schizophreniaQ34487620
P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cellsQ34538994
Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PETQ34572780
Consensus nomenclature for in vivo imaging of reversibly binding radioligandsQ34630958
The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).Q36015358
Drug resistance in epilepsy: putative neurobiologic and clinical mechanismsQ36157234
P-glycoprotein function at the blood-brain barrier: effects of age and genderQ36382013
Pharmacokinetic modeling of P-glycoprotein function at the rat and human blood-brain barriers studied with (R)-[11C]verapamil positron emission tomographyQ36462753
Decreased blood-brain barrier P-glycoprotein function in the progression of Parkinson's disease, PSP and MSA.Q36772901
A comparative small-animal PET evaluation of [11C]tariquidar, [11C]elacridar and (R)-[11C]verapamil for detection of P-glycoprotein-expressing murine breast cancerQ36935382
Age dependency of cerebral P-gp function measured with (R)-[11C]verapamil and PET.Q36947632
A pilot study to assess the efficacy of tariquidar to inhibit P-glycoprotein at the human blood-brain barrier with (R)-11C-verapamil and PETQ36949068
Synthesis and preclinical evaluation of the radiolabeled P-glycoprotein inhibitor [(11)C]MC113.Q36949082
Synthesis and in vivo evaluation of [11C]tariquidar, a positron emission tomography radiotracer based on a third-generation P-glycoprotein inhibitorQ36949086
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 barrierQ36949089
Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET.Q36949815
Tariquidar-induced P-glycoprotein inhibition at the rat blood-brain barrier studied with (R)-11C-verapamil and PET.Q36949854
PET and SPECT radiotracers to assess function and expression of ABC transporters in vivoQ36953090
A novel positron emission tomography imaging protocol identifies seizure-induced regional overactivity of P-glycoprotein at the blood-brain barrierQ36955931
On the rate and extent of drug delivery to the brain.Q37023904
Immuno-PET: a navigator in monoclonal antibody development and applications.Q37047713
Development of inhibitors of ATP-binding cassette drug transporters: present status and challengesQ37076348
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp functionQ37105870
P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeysQ37120685
The antiepileptic drug mephobarbital is not transported by P-glycoprotein or multidrug resistance protein 1 at the blood-brain barrier: a positron emission tomography studyQ37185659
Synthesis of 11C, 18F, 15O, and 13N radiolabels for positron emission tomography.Q37318975
Imaging the function of P-glycoprotein with radiotracers: pharmacokinetics and in vivo applicationsQ37353400
Imaging of cyclosporine inhibition of P-glycoprotein activity using 11C-verapamil in the brain: studies of healthy humansQ37369295
Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoproteinQ37474224
Using PET studies of P-gp function to elucidate mechanisms underlying the disposition of drugs.Q37774380
Carbon-11 labeled tracers for in vivo imaging P-glycoprotein function: kinetics, advantages and disadvantages.Q37774382
Three decades of P-gp inhibitors: skimming through several generations and scaffolds.Q37976863
Evaluation of the P-glycoprotein- and breast cancer resistance protein-mediated brain penetration of 11C-labeled topotecan using small-animal positron emission tomographyQ39515213
Validation of tomographic measurement of cerebral blood volume with C-11-labeled carboxyhemoglobinQ39712316
Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs.Q39855572
LRP/amyloid beta-peptide interaction mediates differential brain efflux of Abeta isoforms.Q40528558
(R)- and (S)-[11C]verapamil as PET-tracers for measuring P-glycoprotein function: in vitro and in vivo evaluation.Q40633547
Evaluation of 11C-colchicine for PET imaging of multiple drug resistance.Q40774166
Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoproteinQ40885386
Carbon-11-labeled daunorubicin and verapamil for probing P-glycoprotein in tumors with PET.Q41172348
Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier.Q41823653
P-glycoprotein deficiency at the blood-brain barrier increases amyloid-beta deposition in an Alzheimer disease mouse modelQ41844698
[11C]Flumazenil brain uptake is influenced by the blood-brain barrier efflux transporter P-glycoproteinQ42153842
[11C]phenytoin revisited: synthesis by [11C]CO carbonylation and first evaluation as a P-gp tracer in ratsQ42354388
Regional increase in P-glycoprotein function in the blood-brain barrier of patients with chronic schizophrenia: a PET study with [(11)C]verapamil as a probe for P-glycoprotein functionQ42974372
Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET.Q43111234
Comment regarding Bergmann et al.'s "Assessment of the in vitro and in vivo properties of a 99mTc-labeled inhibitor of the multidrug resistant gene product of P-glycoprotein".Q44454372
Quantitative assessment of P-glycoprotein function in the rat blood-brain barrier by distribution volume of [11C]verapamil measured with PET.Q44671680
Comparison of in vitro and in vivo models of drug transcytosis through the blood-brain barrierQ44748118
Synthesis and preclinical evaluation of novel PET probes for P-glycoprotein function and expression.Q45967469
In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [(11)C]gefitinibQ46073165
Noninvasive and quantitative assessment of the function of multidrug resistance-associated protein 1 in the living brainQ46264183
Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomographyQ46551897
Synthesis and evaluation of dopamine D3 receptor antagonist 11C-GR218231 as PET tracer for P-glycoproteinQ46639262
Pharmacokinetics of P-glycoprotein inhibition in the rat blood-brain barrierQ46668112
Blood-brain barrier P-glycoprotein function decreases in specific brain regions with aging: a possible role in progressive neurodegenerationQ46688887
Blood-brain barrier P-glycoprotein function is not impaired in early Parkinson's disease.Q46714452
A method for the synthesis of an oseltamivir PET tracer.Q46869398
Imaging of P-glycoprotein-mediated pharmacoresistance in the hippocampus: proof-of-concept in a chronic rat model of temporal lobe epilepsy.Q48127121
Pharmacoresistance in epilepsy: a pilot PET study with the P-glycoprotein substrate R-[(11)C]verapamilQ48176609
Altered GABAA receptor density and unaltered blood-brain barrier transport in a kainate model of epilepsy: an in vivo study using 11C-flumazenil and PET.Q48300046
Effect of a P-glycoprotein inhibitor, Cyclosporin A, on the disposition in rodent brain and blood of the 5-HT1A receptor radioligand, [11C](R)-(-)-RWAY.Q48363502
Comparison of bolus and infusion methods for receptor quantitation: application to [18F]cyclofoxy and positron emission tomographyQ48370689
Quantification of serotonin 5-HT1A receptors in monkey brain with [11C](R)-(-)-RWAY.Q48429445
Symptom provocation in specific phobia affects the substance P neurokinin-1 receptor systemQ48430375
Cerebral blood flow, blood volume, and brain tissue hematocrit during isovolemic hemodilution with hetastarch in ratsQ48463932
Duration and degree of cyclosporin induced P-glycoprotein inhibition in the rat blood-brain barrier can be studied with PET.Q48466700
Deposition of Alzheimer's beta-amyloid is inversely correlated with P-glycoprotein expression in the brains of elderly non-demented humansQ48476417
P433issue2
P921main subjectblood–brain barrierQ221694
P304page(s)225-237
P577publication date2012-12-04
P1433published inACS Chemical NeuroscienceQ2819059
P1476titleAdvances in PET imaging of P-glycoprotein function at the blood-brain barrier
P478volume4

Reverse relations

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