Monoacylglycerol Lipase Inhibition in Tourette Syndrome: A 12‐Week, Randomized, Controlled Study
Sign Up to like & getrecommendations! Published in 2021 at "Movement Disorders"
DOI: 10.1002/mds.28681
Abstract: Modulation of the endocannabinoid system via monoacylglycerol lipase inhibition with Lu AG06466 (formerly known as ABX‐1431) has previously been shown to reduce tics in patients with Tourette syndrome. read more here.
Keywords: monoacylglycerol lipase; syndrome week; inhibition tourette; lipase inhibition ... See more keywords
Development of High Brain-Penetrant and Reversible Monoacylglycerol Lipase PET Tracers for Neuroimaging.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01706
Abstract: 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 diseases. In this study, we designed and… read more here.
Keywords: monoacylglycerol lipase; brain; pet; high brain ... See more keywords
Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.1c01806
Abstract: Monoacylglycerol lipase (MAGL) is the enzyme responsible for the metabolism of 2-arachidonoylglycerol in the brain and the hydrolysis of peripheral monoacylglycerols. Many studies demonstrated beneficial effects deriving from MAGL inhibition for neurodegenerative diseases, inflammatory pathologies,… read more here.
Keywords: new class; monoacylglycerol lipase; class; class benzylpiperidine ... See more keywords
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01531
Abstract: Monoacylglycerol lipase (MAGL) is the main enzyme responsible for degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the CNS. MAGL catalyzes the conversion of 2-AG to arachidonic acid (AA), a precursor to the proinflammatory eicosannoids such… read more here.
Keywords: monoacylglycerol lipase; chemistry; piperidine carbamates; magl ... See more keywords
Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00824
Abstract: Monoacylglycerol lipase (MAGL) is a major serine hydrolase that hydrolyzes 2-arachidonoylglycerol (2-AG) to arachidonic acid (AA) and glycerol in the brain. Because 2-AG and AA are endogenous biologically active ligands in the brain, inhibition of… read more here.
Keywords: piperazinyl pyrrolidin; pyrrolidin ones; piperazinyl; monoacylglycerol lipase ... See more keywords
Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00951
Abstract: The serine hydrolase monoacylglycerol lipase (MGLL) converts the endogenous cannabinoid receptor agonist 2-arachidonoylglycerol (2-AG) and other monoacylglycerols into fatty acids and glycerol. Genetic or pharmacological inactivation of MGLL leads to elevation in 2-AG in the… read more here.
Keywords: mgll; abx 1431; inhibitor; monoacylglycerol lipase ... See more keywords
Design, Synthesis, and Evaluation of (4 R)-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) as a Novel Positron-Emission Tomography Imaging Agent for Monoacylglycerol Lipase.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01576
Abstract: Monoacylglycerol lipase (MAGL) is a cytosolic serine hydrolase involved in endocannabinoid and inflammatory signaling. Positron-emission tomography (PET) imaging of MAGL serves to validate target engagement of therapeutic MAGL inhibitors as well as to investigate MAGL… read more here.
Keywords: monoacylglycerol lipase; positron emission; 18f fluoro; fluoro ... See more keywords
Identification and development of an irreversible monoacylglycerol lipase (MAGL) positron emission tomography (PET) radioligand with high specificity.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00847
Abstract: Monoacylglycerol lipase (MAGL), a serine hydrolase extensively expressed throughout the brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling. Pre-clinically, inhibition of MAGL is known to provide therapeutic benefits for a number… read more here.
Keywords: pet; monoacylglycerol lipase; emission tomography; lipase magl ... See more keywords
Monoacylglycerol Lipase Modulators for Treating Autism Spectrum Disorders.
Sign Up to like & getrecommendations! Published in 2023 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.3c00121
Abstract: Provided herein are monoacylglycerol lipase modulators, pharmaceutical compositions, use of such compounds in treating autism spectrum disorders and processes for preparing such compounds. read more here.
Keywords: treating autism; autism spectrum; spectrum disorders; monoacylglycerol lipase ... See more keywords
The Monoacylglycerol Lipase Inhibitor ABX-1431 Does Not Improve Alcoholic Liver Disease.
Sign Up to like & getrecommendations! Published in 2023 at "Cannabis and cannabinoid research"
DOI: 10.1089/can.2023.0003
Abstract: Introduction: Excessive alcohol consumption can result in alcoholic liver disease (ALD). There is no FDA-approved drug to specifically treat ALD and current management approaches have limited efficacy. Past studies indicate that monoacylglycerol lipase (MAGL) inhibition… read more here.
Keywords: inhibitor abx; alcoholic liver; monoacylglycerol lipase; abx 1431 ... See more keywords
Expression of monoacylglycerol lipase as a marker of tumour invasion and progression in malignant melanoma
Sign Up to like & getrecommendations! Published in 2017 at "Journal of the European Academy of Dermatology and Venereology"
DOI: 10.1111/jdv.14455
Abstract: Accumulating evidence suggests that the lipid lytic enzyme monoacylglycerol lipase (MAGL) promotes tumour invasion and metastasis through up‐regulation of pro‐tumorigenic signalling lipids in several tumour cell lines. However, the expression status of MAGL in clinical… read more here.
Keywords: melanoma; monoacylglycerol lipase; tumour invasion;