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<i>β</i>-Caryophyllene Inhibits Monoacylglycerol Lipase Activity and Increases 2-Arachidonoyl Glycerol Levels In Vivo: A New Mechanism of Endocannabinoid-Mediated Analgesia? [PDF]

Mol Pharmacol
Klawitter J, Weissenborn W, Gvon I, Walz M, Klawitter J, Jackson M, Sempio C, Joksimovic SL, Shokati T, Just I, Christians U, Todorovic SM.   +11 more
europepmc   +1 more source

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Monoacylglycerol lipase

Neurochemical Pathology, 1984
The presence of monoacylglycerol lipase was established in extracts of acetone-dried powders from rat and bovine brains using thioester substrate analogs. At pH 7.4, the apparent Km and Vmax values for 1-S-decanoyl-1-mercapto-2,3-propanediol were 56 microM and 227 nmol/h/mg protein in bovine gray matter.
Joanna B Strosznajder, L A Horrocks
exaly   +3 more sources

Monoacylglycerol lipase (MAGL) as a promising therapeutic target

Biochemical Pharmacology, 2018
Monoacylglycerol lipase (MAGL) has been characterized as the main enzyme responsible for the inactivation of the most abundant brain endocannabinoid, 2-arachidonoylglycerol (2-AG). Besides this role, MAGL has progressively acquired a growing importance as an integrative metabolic hub that controls not only the in vivo levels of 2-AG but also of other ...
María L López-Rodríguez, Silvia Ortega-Gutiérrez, Mar Martín-Fontecha   +2 more
exaly   +3 more sources

MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS

, 2021
The present invention relates to compounds of formula (I) useful as inhibitors, in particular as reversible non-covalent inhibitors, of the enzyme monoacylglycerol lipase (MAGL). The present invention also relates to the therapeutic use of such compounds,
GRANCHI CARLOTTA, BONONI GIULIA, MACCHIA MARCO, MINUTOLO FILIPPO, POLI GIULIO, SCALABRINI DIANA, TUCCINARDI TIZIANO, RIZZOLIO FLAVIO, GIORDANO ANTONIO   +8 more
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Diacylglycerol breakdown in plasma membranes of bovine chromaffin cells is a two-step mechanism mediated by a diacylglycerol lipase and a monoacylglycerol lipase

Biochimica Et Biophysica Acta - Biomembranes, 1987
The recently identified diacylglycerol lipase activity in membranes of chromaffin cells from bovine adrenal medulla [24] is now shown to consist of two enzymes working in series.
Reist M, Zahler P, Rindlisbacher B
exaly   +2 more sources

Properties of monoacylglycerol lipase in rabbit aorta

Lipids, 1987
AbstractMonoacylglycerol lipase activity was characterized in a soluble preparation from rabbit aorta (intima‐media) obtained by combining a 100,000×g supernatant fraction with activity solubilized from the 100,000×g precipitate fraction by treatment with Triton X‐100.
M, Hee-Cheong, D L, Severson
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Lipase-catalyzed synthesis of monoacylglycerol in a homogeneous system

Biotechnology Letters, 2003
The 1,3-regiospecifique lipase, Lipozyme IM, catalyzed the esterification of lauric acid and glycerol in a homogeneous system. To overcome the drawback of the insolubility of glycerol in hexane, which is extensively used in enzymatic synthesis, a mixture of n-hexane/tert-butanol (1:1, v/v) was used leading to a monophasic system.
Julieta B, Monteiro, Maria G, Nascimento, Jorge L, Ninow   +2 more
openaire   +2 more sources

A Review on the Monoacylglycerol Lipase: At the Interface Between Fat and Endocannabinoid Signalling

Current Medicinal Chemistry, 2010
Together with anandamide, 2-arachidonoylglycerol (2-AG) constitutes one of the main representatives of a family of endogenous lipids known as endocannabinoids. These act by binding to CB(1) and CB(2) cannabinoid receptors, the molecular target of the psychoactive compound Delta(9)-THC, both in the periphery and in the central nervous system, where they
Labar, G., Wouters, J., Lambert, D. M.
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The Medicinal Chemistry of Agents Targeting Monoacylglycerol Lipase

Current Topics in Medicinal Chemistry, 2008
Monoacylglycerol lipase (MAGL) has been recently proposed as the main enzymatic activity responsible for the in vivo hydrolysis of the most abundant endocannabinoid in the brain, the 2-arachidonoylglycerol (2-AG). The endocannabinoids, mainly anandamide (AEA) and 2-AG, are a class of lipid messengers that modulate a broad number of physiological ...
Alma, Viso, José A, Cisneros, Silvia, Ortega-Gutiérrez   +2 more
openaire   +2 more sources