Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity.
Animals
Binding Sites
Brain
/ diagnostic imaging
Carbamates
/ pharmacology
Dogs
Drug Design
Endocannabinoids
/ metabolism
Enzyme Inhibitors
/ pharmacology
Humans
Ligands
Madin Darby Canine Kidney Cells
Magnetic Resonance Imaging
Monoacylglycerol Lipases
/ chemistry
Positron-Emission Tomography
Rats
Rats, Sprague-Dawley
Solvents
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:
26 09 2019
26 09 2019
Historique:
pubmed:
5
9
2019
medline:
23
6
2020
entrez:
5
9
2019
Statut:
ppublish
Résumé
Monoacylglycerol lipase (MAGL), a serine hydrolase extensively expressed throughout the brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling. Preclinically, inhibition of MAGL is known to provide therapeutic benefits for a number of neurological disorders. The availability of a MAGL-specific positron emission tomography (PET) ligand would considerably facilitate the development and clinical characterization of MAGL inhibitors via noninvasive and quantitative PET imaging. Herein, we report the identification of the potent and selective irreversible MAGL inhibitor
Identifiants
pubmed: 31483137
doi: 10.1021/acs.jmedchem.9b00847
doi:
Substances chimiques
Carbamates
0
Endocannabinoids
0
Enzyme Inhibitors
0
Ligands
0
Solvents
0
Monoacylglycerol Lipases
EC 3.1.1.23
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM