Using in vitro measurements of plasma and tissue free fractions to interpret radioligand uptake

R Gunn, S Summerfield, C Salinas, K Read, G Searle… - 2007 - Soc Nuclear Med
1141 Objectives: Until recently, passive diffusion across the BBB has been a general
assumption for transport of PET radioligands into the brain. To account for active transport …

Quantification of translocator protein (18 kDa) in the human brain with PET and a novel radioligand, 18F-PBR06

Y Fujimura, SS Zoghbi, FG Simeon… - Journal of Nuclear …, 2009 - Soc Nuclear Med
Translocator protein (TSPO)(18 kDa), formerly called the peripheral benzodiazepine
receptor, is upregulated on activated microglia and macrophages and is, thus, a biomarker …

[PDF][PDF] PET Quantification in Molecular Brain Imaging Taking into Account the Contribution of the Radiometabolite Entering the Brain

M Ichise, Y Kimura, H Shimada… - … on Nuclear Medicine …, 2016 - library.oapen.org
A good understanding of the in vivo pharmacokinetics of radioligands is important for
accurate PET quantification in molecular brain imaging. For many reversibly binding …

Evaluation of reference tissue models for quantification of [11C] Pittsburgh compound B dynamic PET studies

Y Zhou, S Resnick, W Ye, H Fan, D Holt, W Klunk… - 2006 - Soc Nuclear Med
334 Objectives: To compare the performance of three reference tissue models (RTMs) and
parameter estimation algorithms for quantification of [11 C] Pittsburgh compound B ([11 C] …

In vitro equilibrium partitioning in blood cells to measure plasma free fraction of PET radioligands

A Kowalski, C Morse, M Fujita, V Pike, R Innis… - 2016 - Soc Nuclear Med
401 Objectives Ultrafiltration is the most common method of determining plasma free fraction
(f P) for brain PET radioligands (ratio of free concentration to free plus protein-bound …

Avoiding barriers to PET radioligand development: cellular assays of brain efflux transporters

MD Hall, VW Pike - Journal of Nuclear Medicine, 2011 - Soc Nuclear Med
PET provides a uniquely sensitive and powerful means for studying a clinically relevant
protein target within the brain, provided that an adequately specific and sensitive radiotracer …

Assessment of cerebral P-glycoprotein expression and function with PET by combined [11C] inhibitor and [11C] substrate scans in rats

J Müllauer, R Karch, JP Bankstahl, M Bankstahl… - Nuclear Medicine and …, 2013 - Elsevier
Introduction The adenosine triphosphate-binding cassette (ABC) transporter P-glycoprotein
(Pgp) protects the brain from accumulation of lipophilic compounds by active efflux transport …

[PDF][PDF] Predictive in vitro methods in experimental nuclear medicine: Blood Brain Barrier Penetration

C Vraka - 2017 - phaidra.univie.ac.at
The incidence of neurological diseases increases perpetually, on the one hand, due to the
rising incidence of psychiatric diseases in young people and on the other hand due to an …

Compartmental model with plasma input versus reference tissue model for quantification of ligand-receptor dynamic PET studies

Y Zhou, W Ye, J Brasic, J Hilton, D Wong - 2006 - Soc Nuclear Med
335 Objectives: To evaluate three reference tissue models (RTMs) as compared to the
compartmental model with plasma input for quantification of ligand-receptor dynamic PET …

Test–retest reproducibility of 18F-MPPF PET in healthy humans: a reliability study

N Costes, L Zimmer, A Reilhac, F Lavenne… - Journal of Nuclear …, 2007 - Soc Nuclear Med
The aim of this study was to assess the reliability of 2′-methoxyphenyl-(N-2′-pyridinyl)-p-
18F-fluoro-benzamidoethylpiperazine (18F-MPPF) PET binding parameter's quantification …