Comparison of [11C]-(R)-PK 11195 and [11C] PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: implications for positron emission …

…, J Hong, CL Morse, SS Zoghbi, RL Gladding… - Neuroimage, 2010 - Elsevier
Ten percent of humans lack specific binding of [ 11 C]PBR28 to 18 kDa translocator protein (TSPO),
a biomarker for inflammation. “Non-binders” have not been reported using another …

[HTML][HTML] The PET radioligand [11C] MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain

…, AK Chesterfield, CC Felder, RL Gladding… - …, 2008 - nature.com
The cannabinoid CB 1 receptor is one of the most abundant G protein-coupled receptors in
the brain and is a promising target of therapeutic drug development. Success of drug …

Synthesis and evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single …

…, Y Zhang, KJ Jenko, RL Gladding… - ACS chemical …, 2014 - ACS Publications
The imaging of translocator 18 kDa protein (TSPO) in living human brain with radioligands
by positron emission tomography (PET) has become an important means for the study of …

[HTML][HTML] PET measurement of cyclooxygenase-2 using a novel radioligand: upregulation in primate neuroinflammation and first-in-human study

…, JA Montero Santamaria, RL Gladding… - Journal of …, 2020 - Springer
Background Cyclooxygenase-2 (COX-2), which is rapidly upregulated by inflammation, is a
key enzyme catalyzing the rate-limiting step in the synthesis of several inflammatory …

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

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

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

…, E Tuan, N Lazarova, RL Gladding… - 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 11 C-…

Evaluation of two potent and selective PET radioligands to image COX-1 and COX-2 in rhesus monkeys

…, P Singh, C Morse, JS Liow, RL Gladding… - Journal of Nuclear …, 2018 - Soc Nuclear Med
This study assessed whether the newly developed PET radioligands 11 C-PS13 and 11 C-MC1
could image constitutive levels of cyclooxygenase (COX)-1 and COX-2, respectively, in …

Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising 18F-Labeled Ligand

…, LS Manly, JS Liow, RL Gladding… - Journal of medicinal …, 2021 - ACS Publications
Translocator protein 18 kDa (TSPO) is a biomarker of neuroinflammation. [ 11 C]ER176
robustly quantifies TSPO in the human brain with positron emission tomography (PET), …

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

…, P Herscovitch, K Jenko, RL Gladding… - 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 …

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

…, N Lazarova, N Seneca, RL Gladding… - Journal of nuclear …, 2009 - Soc Nuclear Med
11 C-Loperamide is an avid substrate for P-glycoprotein (P-gp), but it is rapidly metabolized
to 11 C-N-desmethyl-loperamide ( 11 C-dLop), which is also a substrate for P-gp and …