Monoacylglycerol lipase (MAGL) as a promising therapeutic target

A Gil-Ordóñez, M Martín-Fontecha… - Biochemical …, 2018 - Elsevier
Monoacylglycerol lipase (MAGL) has been characterized as the main enzyme responsible
for the inactivation of the most abundant brain endocannabinoid, 2-arachidonoylglycerol (2 …

Positron emission tomography imaging of the endocannabinoid system: opportunities and challenges in radiotracer development

L Hou, J Rong, A Haider, D Ogasawara… - Journal of medicinal …, 2020 - ACS Publications
The endocannabinoid system (ECS) is involved in a wide range of biological functions and
comprises cannabinoid receptors and enzymes responsible for endocannabinoid synthesis …

Identification of ABX-1431, a selective inhibitor of monoacylglycerol lipase and clinical candidate for treatment of neurological disorders

JS Cisar, OD Weber, JR Clapper… - Journal of medicinal …, 2018 - ACS Publications
The serine hydrolase monoacylglycerol lipase (MGLL) converts the endogenous
cannabinoid receptor agonist 2-arachidonoylglycerol (2-AG) and other monoacylglycerols …

2-Arachidonoylglycerol modulation of anxiety and stress adaptation: from grass roots to novel therapeutics

G Bedse, MN Hill, S Patel - Biological psychiatry, 2020 - Elsevier
Over the past decade there has been a surge of interest in the development of
endocannabinoid-based therapeutic approaches for the treatment of diverse …

Development of high brain-penetrant and reversible monoacylglycerol lipase PET tracers for neuroimaging

Y He, M Schild, U Grether, J Benz… - Journal of medicinal …, 2022 - ACS Publications
Monoacylglycerol lipase (MAGL) is one of the key enzymes in the endocannabinoid system.
Inhibition of MAGL has been proposed as an attractive approach for the treatment of various …

Design, synthesis, and evaluation of reversible and irreversible monoacylglycerol lipase positron emission tomography (PET) tracers using a “tail switching” strategy …

Z Chen, W Mori, X Deng, R Cheng… - Journal of medicinal …, 2019 - ACS Publications
Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol
(2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as …

In Vitro and in Vivo Evaluation of 11C-Labeled Azetidinecarboxylates for Imaging Monoacylglycerol Lipase by PET Imaging Studies

R Cheng, W Mori, L Ma, M Alhouayek… - Journal of medicinal …, 2018 - ACS Publications
Monoacylglycerol lipase (MAGL) is the principle enzyme for metabolizing endogenous
cannabinoid ligand 2-arachidonoyglycerol (2-AG). Blockade of MAGL increases 2-AG …

Identification and development of an irreversible monoacylglycerol lipase (MAGL) positron emission tomography (PET) radioligand with high specificity

L Zhang, CR Butler, KP Maresca… - Journal of Medicinal …, 2019 - ACS Publications
Monoacylglycerol lipase (MAGL), a serine hydrolase extensively expressed throughout the
brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling …

Design, Synthesis, and Evaluation of 18F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes

Z Chen, W Mori, H Fu, MA Schafroth… - Journal of medicinal …, 2019 - ACS Publications
Dysfunction of monoacylglycerol lipase (MAGL) is associated with several
psychopathological disorders, including drug addiction and neurodegenerative diseases …

Design, Synthesis, and Evaluation of (4R)-1-{3-[2-(18F)Fluoro-4-methylpyridin-3-yl]phenyl}-4-[4-(1,3-thiazol-2-ylcarbonyl)piperazin-1-yl]pyrrolidin-2-one ([18F]T-401 …

Y Hattori, K Aoyama, J Maeda, N Arimura… - Journal of medicinal …, 2019 - ACS Publications
Monoacylglycerol lipase (MAGL) is a cytosolic serine hydrolase involved in
endocannabinoid and inflammatory signaling. Positron-emission tomography (PET) imaging …