Evaluation of two potent and selective PET radioligands to image COX-1 and COX-2 in rhesus monkeys
MJ Kim, SS Shrestha, M Cortes, P Singh… - Journal of Nuclear …, 2018 - Soc Nuclear Med
This study assessed whether the newly developed PET radioligands 11C-PS13 and 11C-
MC1 could image constitutive levels of cyclooxygenase (COX)-1 and COX-2, respectively, in …
MC1 could image constitutive levels of cyclooxygenase (COX)-1 and COX-2, respectively, in …
Novel PET radioligands show that, in rhesus monkeys, COX-1 is constitutively expressed and COX-2 is induced by inflammation
203 Objectives: The cyclooxygenase (COX) system comprises two primary isoforms, COX-1
and COX-2, which regulate the rate-limiting step in the synthesis of prostaglandins and …
and COX-2, which regulate the rate-limiting step in the synthesis of prostaglandins and …
First-in-human evaluation of [11C]PS13, a novel PET radioligand, to quantify cyclooxygenase-1 in the brain
Purpose This study assessed whether the newly developed PET radioligand [11 C] PS13,
which has shown excellent in vivo selectivity in previous animal studies, could be used to …
which has shown excellent in vivo selectivity in previous animal studies, could be used to …
Radiosynthesis, in vitro validation, and in vivo evaluation of 18F-labeled COX-1 and COX-2 inhibitors
TJ McCarthy, AU Sheriff, MJ Graneto… - Journal of Nuclear …, 2002 - Soc Nuclear Med
In this article, we describe the radiosynthesis and evaluation of 18F-labeled cyclooxygenase
(COX) inhibitors. 18F-SC63217 is selective to COX-1 and has a COX-1 inhibitory …
(COX) inhibitors. 18F-SC63217 is selective to COX-1 and has a COX-1 inhibitory …
[HTML][HTML] 2-(4-Methylsulfonylphenyl) pyrimidines as prospective radioligands for imaging cyclooxygenase-2 with PET—Synthesis, triage, and radiolabeling
MY Cortes-Salva, S Shrestha, P Singh, CL Morse… - Molecules, 2018 - mdpi.com
Cyclooxygenase 2 (COX-2) is an inducible enzyme responsible for the conversion of
arachidonic acid into the prostaglandins, PGG2 and PGH2. Expression of this enzyme …
arachidonic acid into the prostaglandins, PGG2 and PGH2. Expression of this enzyme …
[HTML][HTML] Progress in PET imaging of neuroinflammation targeting COX-2 enzyme
Neuroinflammation and cyclooxygenase-2 (COX-2) upregulation are associated with the
pathogenesis of degenerative brain diseases such as Alzheimer's disease (AD), Parkinson's …
pathogenesis of degenerative brain diseases such as Alzheimer's disease (AD), Parkinson's …
Synthesis and in vivo evaluation of 18F-desbromo-DuP-697 as a PET tracer for cyclooxygenase-2 expression
EFJ De Vries, A Van Waarde, AR Buursma… - Journal of Nuclear …, 2003 - Soc Nuclear Med
Cyclooxygenase-2 (COX-2) overexpression has been observed in various pathologies, such
as inflammation, cancer, ischemia, and Alzheimer's disease. As an initial step toward a …
as inflammation, cancer, ischemia, and Alzheimer's disease. As an initial step toward a …
Radiosynthesis and in vivo evaluation of [11C] MOV as a PET imaging agent for COX-2
J Prabhakaran, M Underwood, F Zanderigo… - Bioorganic & Medicinal …, 2018 - Elsevier
Radiosynthesis and in vivo evaluation of [11 C] 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-
pyrazol-1-yl] benzenesulfonamide (methoxy analogue of valdecoxib,[11 C] MOV), a COX-2 …
pyrazol-1-yl] benzenesulfonamide (methoxy analogue of valdecoxib,[11 C] MOV), a COX-2 …
Human biodistribution and radiation dosimetry of 11C-(R)-PK11195, the prototypic PET ligand to image inflammation
J Hirvonen, A Roivainen, J Virta, S Helin… - European journal of …, 2010 - Springer
Purpose The positron emission tomography (PET) radiotracer 11 C-(R)-PK11195 allows the
in vivo imaging in humans of the translocator protein 18 kDa (TSPO), previously called …
in vivo imaging in humans of the translocator protein 18 kDa (TSPO), previously called …
3-Substituted 1,5-Diaryl-1H-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 2: Selection and Evaluation of [11C]PS13 for …
S Shrestha, P Singh, MY Cortes-Salva… - ACS chemical …, 2018 - ACS Publications
In our preceding paper (Part 1), we identified three 1, 5-bis-diaryl-1, 2, 4-triazole-based
compounds that merited evaluation as potential positron emission tomography (PET) …
compounds that merited evaluation as potential positron emission tomography (PET) …