11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux.
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Small and Innovative Molecules as New Strategy to Revert MDRPET radiotracers: crossing the blood-brain barrier and surviving metabolismPredicting the outer boundaries of P-glycoprotein (P-gp)-based drug interactions at the human blood-brain barrier based on rat studies.Effects of ketoconazole on the biodistribution and metabolism of [11C]loperamide and [11C]N-desmethyl-loperamide in wild-type and P-gp knockout mice.P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide.N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrierAvoiding barriers to PET radioligand development: cellular assays of brain efflux transportersLysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PETP-glycoprotein-based loperamide-cyclosporine drug interaction at the rat blood-brain barrier: prediction from in vitro studies and extrapolation to humans.Behavioral effects and central nervous system levels of the broadly available κ-agonist hallucinogen salvinorin A are affected by P-glycoprotein modulation in vivo.In vivo evaluation of limiting brain penetration of probes for α(2C)-adrenoceptor using small-animal positron emission tomography.In Vivo Imaging of Human MDR1 Transcription in the Brain and Spine of MDR1-Luciferase Reporter Mice.Bioluminescent imaging of ABCG2 efflux activity at the blood-placenta barrierAdvances in PET imaging of P-glycoprotein function at the blood-brain barrier.Imaging of P-glycoprotein function and expression to elucidate mechanisms of pharmacoresistance in epilepsy.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 barrierPET and SPECT radiotracers to assess function and expression of ABC transporters in vivoA novel positron emission tomography imaging protocol identifies seizure-induced regional overactivity of P-glycoprotein at the blood-brain barrierSynthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp functionP-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeys.Physiologically based pharmacokinetic modelling of drug penetration across the blood-brain barrier--towards a mechanistic IVIVE-based approachOn quantitative relationships between drug-like compound lipophilicity and plasma free fraction in monkey and human.Imaging the function of P-glycoprotein with radiotracers: pharmacokinetics and in vivo applications.Drug interactions at the blood-brain barrier: fact or fantasy?Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoprotein.In vitro, in vivo and in silico models of drug distribution into the brain.Radioligands targeting P-glycoprotein and other drug efflux proteins at the blood-brain barrier.Positron emission tomography radioligands for the opioid system.Novel pre-clinical methodologies for pharmacokinetic drug-drug interaction studies: spotlight on "humanized" animal models.Radiopharmaceuticals for assessing ABC transporters at the blood-brain barrier.Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.Imaging P-glycoprotein function in rats using [(11)C]-N-desmethyl-loperamide.Discrepancies in the P-glycoprotein-mediated transport of (18)F-MPPF: a pharmacokinetic study in mice and non-human primates.Toward an improved prediction of human in vivo brain penetration.Synthesis and In Vivo Imaging of N-(3-[11C]Methoxybenzyl)-2-(3-Methoxyphenyl)ethylaniline as a Potential Targeting Agent for P-glycoprotein.
P2860
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P2860
11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux.
description
2008 nî lūn-bûn
@nan
2008 թուականի Մարտին հրատարակուած գիտական յօդուած
@hyw
2008 թվականի մարտին հրատարակված գիտական հոդված
@hy
2008年の論文
@ja
2008年論文
@yue
2008年論文
@zh-hant
2008年論文
@zh-hk
2008年論文
@zh-mo
2008年論文
@zh-tw
2008年论文
@wuu
name
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@ast
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@en
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@nl
type
label
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@ast
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@en
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@nl
prefLabel
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@ast
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@en
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@nl
P2093
P1476
11C-loperamide and its N-desme ...... meability-glycoprotein efflux.
@en
P2093
Edward Tuan
Fumihiko Yasuno
Jeih-San Liow
Jinsoo Hong
Neva Lazarova
Robert B Innis
Robert L Gladding
Sami S Zoghbi
Victor W Pike
P304
P356
10.2967/JNUMED.107.047308
P407
P577
2008-03-14T00:00:00Z