Radiosynthesis and evaluation of [
Animals
Blood-Brain Barrier
/ metabolism
Brain
/ metabolism
Celecoxib
/ metabolism
Cell Line, Tumor
Cyclooxygenase 2
/ metabolism
Fluorides
/ metabolism
Fluorine Radioisotopes
/ metabolism
Humans
Inflammation
/ metabolism
Ligands
Male
Mice
Mice, Nude
Positron-Emission Tomography
/ methods
Pyridines
/ metabolism
Radiopharmaceuticals
/ metabolism
Brain
COX-2
Inflammation
PET
Radiotracer
Journal
Pharmacological reports : PR
ISSN: 2299-5684
Titre abrégé: Pharmacol Rep
Pays: Switzerland
ID NLM: 101234999
Informations de publication
Date de publication:
Oct 2020
Oct 2020
Historique:
received:
06
04
2020
accepted:
25
06
2020
revised:
22
06
2020
pubmed:
8
7
2020
medline:
3
7
2021
entrez:
8
7
2020
Statut:
ppublish
Résumé
The upregulation of cyclooxygenase-2 (COX-2) is involved in neuroinflammation associated with many neurological diseases as well as cancers of the brain. Outside the brain, inflammation and COX-2 induction contribute to the pathogenesis of pain, arthritis, acute allograft rejection, and in response to infections, tumors, autoimmune disorders, and injuries. Herein, we report the radiochemical synthesis and evaluation of [ The radiochemical synthesis of [ A twofold higher binding of [ Specific binding to COX-2 in BxPC3 cell lines, BBB permeability, and increased brain uptake in neuroinflammation mice qualifies [
Sections du résumé
BACKGROUND
BACKGROUND
The upregulation of cyclooxygenase-2 (COX-2) is involved in neuroinflammation associated with many neurological diseases as well as cancers of the brain. Outside the brain, inflammation and COX-2 induction contribute to the pathogenesis of pain, arthritis, acute allograft rejection, and in response to infections, tumors, autoimmune disorders, and injuries. Herein, we report the radiochemical synthesis and evaluation of [
METHODS
METHODS
The radiochemical synthesis of [
RESULTS
RESULTS
A twofold higher binding of [
CONCLUSIONS
CONCLUSIONS
Specific binding to COX-2 in BxPC3 cell lines, BBB permeability, and increased brain uptake in neuroinflammation mice qualifies [
Identifiants
pubmed: 32632914
doi: 10.1007/s43440-020-00124-z
pii: 10.1007/s43440-020-00124-z
doi:
Substances chimiques
(4-(4-fluorophenyl)-1-methyl-1,2,3,6-tetrahydropyridine)
0
Fluorine Radioisotopes
0
Ligands
0
Pyridines
0
Radiopharmaceuticals
0
Cyclooxygenase 2
EC 1.14.99.1
Fluorine-18
GZ5I74KB8G
Celecoxib
JCX84Q7J1L
Fluorides
Q80VPU408O
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM