P-glycoprotein function at the blood–brain barrier imaged using 11C-N-desmethyl-loperamide in monkeys

JS Liow, W Kreisl, SS Zoghbi, N Lazarova… - Journal of nuclear …, 2009 - Soc Nuclear Med
11C-Loperamide is an avid substrate for P-glycoprotein (P-gp), but it is rapidly metabolized
to 11C-N-desmethyl-loperamide (11C-dLop), which is also a substrate for P-gp and thereby …

Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoprotein

N Seneca, SS Zoghbi, JS Liow, W Kreisl… - Journal of nuclear …, 2009 - Soc Nuclear Med
P-glycoprotein (P-gp) is a membrane-bound efflux pump that limits the distribution of drugs
to several organs of the body. At the blood–brain barrier, P-gp blocks the entry of both …

11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux

SS Zoghbi, JS Liow, F Yasuno, J Hong… - Journal of nuclear …, 2008 - Soc Nuclear Med
Loperamide, an opiate receptor agonist, does not cross the blood–brain barrier because it is
a substrate for the permeability-glycoprotein (P-gp) efflux pump. We evaluated 11C …

P-glycoprotein function at the blood–brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide

WC Kreisl, JS Liow, N Kimura, N Seneca… - Journal of Nuclear …, 2010 - Soc Nuclear Med
Permeability-glycoprotein (P-gp), an efflux transporter in several organs, acts at the blood–
brain barrier to protect the brain from exogenous toxins. P-gp almost completely blocks brain …

Effects of ketoconazole on the biodistribution and metabolism of [11C] loperamide and [11C] N-desmethyl-loperamide in wild-type and P-gp knockout mice

N Seneca, SS Zoghbi, HU Shetty, E Tuan… - Nuclear medicine and …, 2010 - Elsevier
INTRODUCTION:[11C] Loperamide and [11C] N-desmethyl-loperamide ([11C] dLop) have
been proposed as radiotracers for imaging brain P-glycoprotein (P-gp) function. A major …

The influence of mass of [11C]-laniquidar and [11C]-N-desmethyl-loperamide on P-glycoprotein blockage at the blood–brain barrier

L Moerman, C Dumolyn, P Boon, F De Vos - Nuclear medicine and biology, 2012 - Elsevier
INTRODUCTION: An earlier report suggested that mass amount of PET tracers could be an
important factor in brain uptake mediated by P-glycoprotein. Thereby, this study investigated …

Increased permeability-glycoprotein inhibition at the human blood–brain barrier can be safely achieved by performing PET during peak plasma concentrations of …

WC Kreisl, R Bhatia, CL Morse, AE Woock… - Journal of Nuclear …, 2015 - Soc Nuclear Med
The permeability-glycoprotein (P-gp) efflux transporter is densely expressed at the blood–
brain barrier, and its resultant spare capacity requires substantial blockade to increase the …

In vivo evaluation of P-glycoprotein modulation of 8 PET radioligands used clinically

K Ishiwata, K Kawamura, K Yanai… - Journal of Nuclear …, 2007 - Soc Nuclear Med
P-glycoprotein (P-gp) regulates the ability of endogenous and exogenous compounds to
cross the blood–brain barrier. We investigated whether PET tracers used clinically for …

Synthesis and Evaluation of [N-methyl-11C]N-Desmethyl-loperamide as a New and Improved PET Radiotracer for Imaging P-gp Function

N Lazarova, SS Zoghbi, J Hong, N Seneca… - Journal of medicinal …, 2008 - ACS Publications
[11C] Loperamide has been proposed for imaging P-glycoprotein (P-gp) function with
positron emission tomography (PET), but its metabolism to [N-methyl-11C] N-desmethyl …

N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier

P Kannan, KR Brimacombe, SS Zoghbi, JS Liow… - Drug Metabolism and …, 2010 - ASPET
[11C] N-desmethyl-Loperamide ([11C] dLop) is used in positron emission tomography (PET)
to measure the in vivo activity of efflux transporters that block the passage of drugs across …