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A reversible and selective inhibitor of monoacylglycerol lipase ameliorates multiple sclerosis
Umeå University, Faculty of Medicine, Department of Pharmacology and Clinical Neuroscience, Pharmacology.
Umeå University, Faculty of Medicine, Department of Pharmacology and Clinical Neuroscience.
Umeå University, Faculty of Medicine, Department of Pharmacology and Clinical Neuroscience, Pharmacology.
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2014 (English)In: Angewandte Chemie International Edition, ISSN 1433-7851, E-ISSN 1521-3773, Vol. 53, no 50, 13765-13770 p.Article in journal (Refereed) Published
Abstract [en]

Monoacylglycerol lipase (MAGL) is the enzyme responsible for the inactivation of the endocannabinoid 2-arachidonoylglycerol (2-AG). MAGL inhibitors show analgesic and tissue-protecting effects in several disease models. However, the few efficient and selective MAGL inhibitors described to date block the enzyme irreversibly, and this can lead to pharmacological tolerance. Hence, additional classes of MAGL inhibitors are needed to validate this enzyme as a therapeutic target. Here we report a potent, selective, and reversible MAGL inhibitor (IC50=0.18M) which is active in vivo and ameliorates the clinical progression of a multiple sclerosis (MS) mouse model without inducing undesirable CB1-mediated side effects. These results support the interest in MAGL as a target for the treatment of MS.

Place, publisher, year, edition, pages
Wiley-VCH Verlagsgesellschaft, 2014. Vol. 53, no 50, 13765-13770 p.
Keyword [en]
endocannabinoids, endogenous cannabinoid system, enzyme inhibitors, monoacylglycerol lipase, ltiple sclerosis
National Category
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)
Identifiers
URN: urn:nbn:se:umu:diva-97884DOI: 10.1002/anie.201407807ISI: 000345833100020OAI: oai:DiVA.org:umu-97884DiVA: diva2:781350
Available from: 2015-01-16 Created: 2015-01-08 Last updated: 2017-05-23Bibliographically approved

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Cipriano, MariateresaHedén, ErikaBjörklund, EmmelieFowler, Christopher J.
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PharmacologyDepartment of Pharmacology and Clinical Neuroscience
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Angewandte Chemie International Edition
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)

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