Identification and Preclinical Development of a 2,5,6-Trisubstituted Fluorinated Pyridine Derivative as a Radioligand for the Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors.
Animals
Brain
/ diagnostic imaging
Fluorine Radioisotopes
/ chemistry
Humans
Ligands
Male
Molecular Docking Simulation
Molecular Structure
Positron-Emission Tomography
Pyridines
/ chemical synthesis
Radiopharmaceuticals
/ chemical synthesis
Rats, Wistar
Receptor, Cannabinoid, CB2
/ metabolism
Spinal Cord
/ diagnostic imaging
Spleen
/ diagnostic imaging
Structure-Activity Relationship
Tritium
/ chemistry
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
24 09 2020
24 09 2020
Historique:
pubmed:
14
8
2020
medline:
5
1
2021
entrez:
14
8
2020
Statut:
ppublish
Résumé
Despite the broad implications of the cannabinoid type 2 receptor (CB2) in neuroinflammatory processes, a suitable CB2-targeted probe is currently lacking in clinical routine. In this work, we synthesized 15 fluorinated pyridine derivatives and tested their binding affinities toward CB2 and CB1. With a sub-nanomolar affinity (
Identifiants
pubmed: 32787079
doi: 10.1021/acs.jmedchem.0c00778
doi:
Substances chimiques
Fluorine Radioisotopes
0
Ligands
0
Pyridines
0
Radiopharmaceuticals
0
Receptor, Cannabinoid, CB2
0
Tritium
10028-17-8
Fluorine-18
GZ5I74KB8G
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM